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Showing drug card for Vitamin E (DB00163)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-06-23 18:07:35
Primary Accession Number DB00163
Secondary Accession Number
  • EXPT03227
  • NUTR00061
Name Vitamin E
Drug Type
  • Approved
  • Nutraceutical
  • Small Molecule
Description A generic descriptor for all tocopherols and tocotrienols that exhibit alpha-tocopherol activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of isoprenoids. [PubChem]
Synonyms
  1. Tocopherol
  2. alpha-Tocopherol
Brand Names
  1. Amino-Opti-E
  2. Aquasol E
  3. Daltose
  4. E-200 I.U. Softgels
  5. E-Complex-600
  6. E-Ferol
  7. E-Vitamin succinate
  8. Gordo-Vite E
  9. Vitamin Plus E Softgells
  10. Vitec
Brand Mixtures Not Available
Chemical IUPAC Name (2R)-2,5,7,8-tetramethyl-2-[(4R,8R)-4,8,12-trimethyltridecyl]chroman-6-ol
Chemical Formula C29H50O2
Chemical Structure Structure
CAS Registry Number 59-02-9
InChI Identifier InChI=1/C29H50O2/c1-20(2)12-9-13-21(3)14-10-15-22(4)16-11-18-29(8)19-17-26-25(7)27(30)23(5)24(6)28(26)31-29/h20-22,30H,9-19H2,1-8H3/t21-,22-,29-/m1/s1
InChI Key GVJHHUAWPYXKBD-IEOSBIPEBS
KEGG Drug Not Available
KEGG Compound C02477 Link Image
PubChem Compound 14985 Link Image
PubChem Substance 5492 Link Image
ChEBI ID 18145 Link Image
PharmGKB ID PA451900 Link Image
HET ID VIT Link Image
GenBank ID Not Available
Drug ID Number [DIN] Not Available
RxList Link Not Available
PDRhealth Link http://www.pdrhealth.com/drug_info/nmdrugprofiles/nutsupdrugs/vit_0266.shtml Link Image
Wikipedia Link http://en.wikipedia.org/wiki/Vitamin_E Link Image
FDA Label Not Available
Material Safety Data Sheet (MSDS)
Synthesis Reference Not Available
Average Molecular Weight 430.7061
Monoisotopic Molecular Weight 430.3811
State Liquid
Melting Point 2 oC
Experimental Water Solubility Insoluble in water, but water-dispersible. Source: PhysProp
Predicted Water Solubility 7.04e-06 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 10 Source: PhysProp
Predicted LogP 8.84 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -7.79 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point Not Available
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID 1KPM Link Image
Experimental PDB File Show
Experimental PDB Structure
Isomeric SMILES CC(C)CCC[C@@H](C)CCC[C@@H](C)CCC[C@]1(C)CCC2=C(O1)C(C)=C(C)C(O)=C2C
Canonical SMILES CC(C)CCCC(C)CCCC(C)CCCC1(C)CCC2=C(O1)C(C)=C(C)C(O)=C2C
Drug Category
  • Antioxidants
  • Dietary supplement
  • Micronutrient
  • Vitamins
  • Vitamins/minerals
ATC Codes
AHFS Codes
  • 84:24.12
  • 88:20.00
Indication Vitamin E, known for its antioxidant activities, is protective against cardiovascular disease and some forms of cancer and has also demonstrated immune-enhancing effects. It may be of limited benefit in some with asthma and rheumatoid arthritis. It may be helpful in some neurological diseases including Alzheimer's, some eye disorders including cataracts, and diabetes and premenstrual syndrome. It may also help protect skin from ultraviolet irradiation although claims that it reverses skin aging, enhances male fertility and exercise performance are poorly supported. It may help relieve some muscle cramps.
Pharmacology Vitamin E has antioxidant activity. It may also have anti-atherogenic, antithrombotic, anticoagulant, neuroprotective, antiviral, immunomodulatory, cell membrane-stabilizing and antiproliferative actions. Vitamin E is a collective term used to describe eight separate forms, the best-known form being alpha-tocopherol. Vitamin E is a fat-soluble vitamin and is an important antioxidant. It acts to protect cells against the effects of free radicals, which are potentially damaging by-products of the body's metabolism. Vitamin E is often used in skin creams and lotions because it is believed to play a role in encouraging skin healing and reducing scarring after injuries such as burns. There are three specific situations when a vitamin E deficiency is likely to occur. It is seen in persons who cannot absorb dietary fat, has been found in premature, very low birth weight infants (birth weights less than 1500 grams, or 3½ pounds), and is seen in individuals with rare disorders of fat metabolism. A vitamin E deficiency is usually characterized by neurological problems due to poor nerve conduction. Symptoms may include infertility, neuromuscular impairment, menstrual problems, miscarriage and uterine degradation. Preliminary research has led to a widely held belief that vitamin E may help prevent or delay coronary heart disease. Antioxidants such as vitamin E help protect against the damaging effects of free radicals, which may contribute to the development of chronic diseases such as cancer. It also protects other fat-soluble vitamins (A and B group vitamins) from destruction by oxygen. Low levels of vitamin E have been linked to increased incidence of breast and colon cancer.
Mechanism of Action Although all forms of Vitamin E exhibit antioxidant activity, it is known that the antioxidant activity of vitamin E is not sufficient to explain the vitamin's biological activity.
Vitamin E's anti-atherogenic activity involves the inhibition of the oxidation of LDL and the accumulation of oxLDL in the arterial wall. It also appears to reduce oxLDL-induced apoptosis in human endothelial cells. Oxidation of LDL is a key early step in atherogenesis as it triggers a number of events which lead to the formation of atherosclerotic plaque. In addition, vitamin E inhibits protein kinase C (PKC) activity. PKC plays a role in smooth muscle cell proliferation, and, thus, the inhibition of PKC results in inhibition of smooth muscle cell proliferation, which is involved in atherogenesis.
Vitamin E's antithrombotic and anticoagulant activities involves the downregulation of the expression of intracellular cell adhesion molecule(ICAM)-1 and vascular cell adhesion molecule(VCAM)-1 which lowers the adhesion of blood components to the endothelium. In addition, vitamin E upregulates the expression of cytosolic phospholipase A2 and cyclooxygenase (COX)-1 which in turn enhances the release of prostacyclin. Prostacyclin is a vasodilating factor and inhibitor of platelet aggregation and platelet release. It is also known that platelet aggregation is mediated by a mechanism involving the binding of fibrinogen to the glycoprotein IIb/IIIa (GPIIb/IIIa) complex of platelets. GPIIb/IIIa is the major membrane receptor protein that is key to the role of the platelet aggregation response. GPIIb is the alpha-subunit of this platelet membrane protein. Alpha-tocopherol downregulates GPIIb promoter activity which results in reduction of GPIIb protein expression and decreased platelet aggregation. Vitamin E has also been found in culture to decrease plasma production of thrombin, a protein which binds to platelets and induces aggregation. A metabolite of vitamin E called vitamin E quinone or alpha-tocopheryl quinone (TQ) is a potent anticoagulant. This metabolite inhibits vitamin K-dependent carboxylase, which is a major enzyme in the coagulation cascade.
The neuroprotective effects of vitamin E are explained by its antioxidant effects. Many disorders of the nervous system are caused by oxidative stress. Vitamin E protects against this stress, thereby protecting the nervouse system.
The immunomodulatory effects of Vitamin E have been demonstrated in vitro, where alpha-tocopherol increases mitogenic response of T lymphocytes from aged mice. The mechanism of this response by vitamin E is not well understood, however it has been suggested that vitamin E itself may have mitogenic activity independent of its antioxidant activity.
Lastly, the mechanism of action of vitamin E's antiviral effects (primarily against HIV-1) involves its antioxidant activity. Vitamin E reduces oxidative stress, which is thought to contribute to HIV-1 pathogenesis, as well as to the pathogenesis of other viral infections. Vitamin E also affects membrane integrity and fluidity and, since HIV-1 is a membraned virus, altering membrane fluidity of HIV-1 may interfere with its ability to bind to cell-receptor sites, thus decreasing its infectivity.
Absorption 50 to 80% absorbed from gastrointestinal tract.
Toxicity Not Available
Protein Binding Bound to beta-lipoproteins in blood.
Biotransformation Hepatic.
Half Life Not Available
Dosage Forms
Form Route
Capsule Oral
Cream Topical
Liquid Intramuscular
Liquid Oral
Ointment Topical
Powder Oral
Tablet Oral
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions Not Available
Food Interactions Not Available
Pathways Not Available
General References
  1. Iuliano L, Micheletta F, Maranghi M, Frati G, Diczfalusy U, Violi F: Bioavailability of vitamin E as function of food intake in healthy subjects: effects on plasma peroxide-scavenging activity and cholesterol-oxidation products. Arterioscler Thromb Vasc Biol. 2001 Oct;21(10):E34-7. [PubMed Link Image]
  2. Miller ER 3rd, Pastor-Barriuso R, Dalal D, Riemersma RA, Appel LJ, Guallar E: Meta-analysis: high-dosage vitamin E supplementation may increase all-cause mortality. Ann Intern Med. 2005 Jan 4;142(1):37-46. Epub 2004 Nov 10. [PubMed Link Image]
  3. Poston L, Briley AL, Seed PT, Kelly FJ, Shennan AH: Vitamin C and vitamin E in pregnant women at risk for pre-eclampsia (VIP trial): randomised placebo-controlled trial. Lancet. 2006 Apr 8;367(9517):1145-54. [PubMed Link Image]
  4. Rumbold AR, Crowther CA, Haslam RR, Dekker GA, Robinson JS: Vitamins C and E and the risks of preeclampsia and perinatal complications. N Engl J Med. 2006 Apr 27;354(17):1796-806. [PubMed Link Image]
  5. Horwitt MK, Elliott WH, Kanjananggulpan P, Fitch CD: Serum concentrations of alpha-tocopherol after ingestion of various vitamin E preparations. Am J Clin Nutr. 1984 Aug;40(2):240-5. [PubMed Link Image]
  6. Linus Pauling Institute Link Image
  7. Wikipedia Link Image
  8. PDRhealth Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. Glutathione S-transferase A2
  2. Xanthine dehydrogenase/oxidase
Targets
  1. SEC14-like protein 4
  2. Arachidonate 5-lipoxygenase
  3. SEC14-like protein 2
  4. SEC14-like protein 3
  5. Alpha-tocopherol transfer protein
  6. Protein kinase C beta type
  7. Orphan nuclear receptor PXR
  8. Protein kinase C alpha type
  9. Diacylglycerol kinase alpha
  10. Serine/threonine-protein phosphatase 2A catalytic subunit beta isoform
  11. Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoform
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Glutathione S-transferase A2
Enzyme 1 Gene Name GSTA2
Enzyme 1 SwissProt ID P09210 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P09210|GSTA2_HUMAN Glutathione S-transferase A2 
AEKPKLHYSNIRGRMESIRWLLAAAGVEFEEKFIKSAEDLDKLRNDGYLMFQQVPMVEID
GMKLVQTRAILNYIASKYNLYGKDIKEKALIDMYIEGIADLGEMILLLPFTQPEEQDAKL
ALIQEKTKNRYFPAFEKVLKSHGQDYLVGNKLSRADIHLVELLYYVEELDSSLISSFPLL
KALKTRISNLPTVKKFLQPGSPRKPPMDEKSLEESRKIFRF
Phase 1 Metabolizing Enzyme 2 [top]
Enzyme 2 Name Xanthine dehydrogenase/oxidase
Enzyme 2 Gene Name XDH
Enzyme 2 SwissProt ID P47989 Link Image
Enzyme 2 SNPs SNPJam Report Link Image
Enzyme 2 Protein Sequence >sp|P47989|XDH_HUMAN Xanthine dehydrogenase/oxidase 
TADKLVFFVNGRKVVEKNADPETTLLAYLRRKLGLSGTKLGCGEGGCGACTVMLSKYDRL
QNKIVHFSANACLAPICSLHHVAVTTVEGIGSTKTRLHPVQERIAKSHGSQCGFCTPGIV
MSMYTLLRNQPEPTMEEIENAFQGNLCRCTGYRPILQGFRTFARDGGCCGGDGNNPNCCM
NQKKDHSVSLSPSLFKPEEFTPLDPTQEPIFPPELLRLKDTPRKQLRFEGERVTWIQAST
LKELLDLKAQHPDAKLVVGNTEIGIEMKFKNMLFPMIVCPAWIPELNSVEHGPDGISFGA
ACPLSIVEKTLVDAVAKLPAQKTEVFRGVLEQLRWFAGKQVKSVASVGGNIITASPISDL
NPVFMASGAKLTLVSRGTRRTVQMDHTFFPGYRKTLLSPEEILLSIEIPYSREGEYFSAF
KQASRREDDIAKVTSGMRVLFKPGTTEVQELALCYGGMANRTISALKTTQRQLSKLWKEE
LLQDVCAGLAEELHLPPDAPGGMVDFRCTLTLSFFFKFYLTVLQKLGQENLEDKCGKLDP
TFASATLLFQKDPPADVQLFQEVPKGQSEEDMVGRPLPHLAADMQASGEAVYCDDIPRYE
NELSLRLVTSTRAHAKIKSIDTSEAKKVPGFVCFISADDVPGSNITGICNDETVFAKDKV
TCVGHIIGAVVADTPEHTQRAAQGVKITYEELPAIITIEDAIKNNSFYGPELKIEKGDLK
KGFSEADNVVSGEIYIGGQEHFYLETHCTIAVPKGEAGEMELFVSTQNTMKTQSFVAKML
GVPANRIVVRVKRMGGGFGGKETRSTVVSTAVALAAYKTGRPVRCMLDRDEDMLITGGRH
PFLARYKVGFMKTGTVVALEVDHFSNVGNTQDLSQSIMERALFHMDNCYKIPNIRGTGRL
CKTNLPSNTAFRGFGGPQGMLIAECWMSEVAVTCGMPAEEVRRKNLYKEGDLTHFNQKLE
GFTLPRCWEECLASSQYHARKSEVDKFNKENCWKKRGLCIIPTKFGISFTVPFLNQAGAL
LHVYTDGSVLLTHGGTEMGQGLHTKMVQVASRALKIPTSKIYISETSTNTVPNTSPTAAS
VSADLNGQAVYAACQTILKRLEPYKKKNPSGSWEDWVTAAYMDTVSLSATGFYRTPNLGY
SFETNSGNPFHYFSYGVACSEVEIDCLTGDHKNLRTDIVMDVGSSLNPAIDIGQVEGAFV
QGLGLFTLEELHYSPEGSLHTRGPSTYKIPAFGSIPIEFRVSLLRDCPNKKAIYASKAVG
EPPLFLAASIFFAIKDAIRAARAQHTGNNVKELFRLDSPATPEKIRNACVDKFTTLCVTG
VPENCKPWSVRV
Drug Target 1 [top]
Target 1 ID 86
Target 1 Name SEC14-like protein 4
Target 1 Synonyms
  1. Tocopherol-associated protein 3
Target 1 Gene Name SEC14L4
Target 1 Protein Sequence >SEC14-like protein 4 
MSSRVGDLSPQQQEALARFRENLQDLLPILPNADDYFLLRWLRARNFDLQKSEDMLRRHM
EFRKQQDLDNIVTWQPPEVIQLYDSGGLCGYDYEGCPVYFNIIGSLDPKGLLLSASKQDM
IRKRIKVCELLLHECELQTQKLGRKIEMALMVFDMEGLSLKHLWKPAVEVYQQFFSILEA
NYPETLKNLIVIRAPKLFPVAFNLVKSFMSEETRRKIVILGDNWKQELTKFISPDQLPVE
FGGTMTDPDGNPKCLTKINYGGEVPKSYYLCEQVRLQYEHTRSVGRGSSLQVENEILFPG
CVLRWQFASDGGDIGFGVFLKTKMGEQQSAREMTEVLPSQRYNAHMVPEDGSLTCLQAGV
YVLRFDNTYSRMHAKKLSYTVEVLLPDKASEETLQSLKAMRPSPTQ
Target 1 Number of Residues 412
Target 1 Molecular Weight 46644
Target 1 Theoretical pI 6.52
Target 1 GO Classification
Function
carrier activity
protein carrier activity
transporter activity
Process
protein transport
intracellular protein transport
physiological process
cellular physiological process
transport
Component
membrane
cell
intracellular
Target 1 General Function Involved in hydrophobic molecule transport activity
Target 1 Specific Function Probable hydrophobic ligand-binding protein; may play a role in the transport of hydrophobic ligands like tocopherol, squalene and phospholipids
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • None
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 27803380 Link Image
Target 1 UniProtKB/Swiss-Prot ID Q9UDX3 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name S14L4_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location Not Available
Target 1 Gene Sequence >1221 bp 
ATGAGCAGCCGAGTCGGGGACCTGAGCCCCCAGCAGCAGGAAGCGCTGGCCAGGTTCCGG
GAGAACCTCCAGGACCTGCTGCCCATACTGCCCAATGCTGATGACTACTTCCTCCTGCGC
TGGCTGCGAGCTCGAAACTTTGACCTGCAGAAATCCGAAGACATGCTCCGAAGGCACATG
GAGTTCCGGAAGCAACAAGACCTGGACAACATTGTCACATGGCAGCCCCCTGAGGTCATC
CAGCTGTATGACTCGGGTGGTCTTTGTGGCTACGACTACGAAGGCTGCCCTGTGTACTTC
AACATCATTGGGTCCCTCGACCCCAAGGGTCTCCTGCTGTCAGCCTCCAAGCAGGATATG
ATCCGGAAGCGCATCAAAGTCTGTGAGCTGCTGTTGCATGAGTGTGAGCTGCAAACTCAG
AAGCTGGGCAGGAAGATCGAGATGGCGCTGATGGTGTTTGACATGGAGGGGCTGAGCCTG
AAACACCTGTGGAAGCCAGCTGTGGAGGTCTACCAGCAGTTTTTTAGCATCCTGGAAGCA
AATTATCCTGAGACCCTGAAGAATTTAATTGTTATTCGAGCCCCAAAACTGTTCCCCGTG
GCCTTCAACTTGGTCAAGTCGTTCATGAGTGAGGAGACACGCAGGAAGATTGTGATTCTG
GGAGACAACTGGAAGCAGGAGCTGACAAAATTCATCAGCCCCGACCAGCTGCCTGTGGAG
TTTGGGGGGACCATGACTGACCCCGATGGCAACCCCAAGTGCCTGACCAAGATCAACTAT
GGGGGTGAGGTGCCCAAGAGCTACTACCTGTGCGAGCAGGTGAGGCTGCAGTATGAGCAC
ACGAGGTCCGTGGGCCGCGGCTCCTCCCTGCAGGTGGAGAACGAGATCCTGTTCCCGGGC
TGTGTGCTCAGGTGGCAGTTTGCTTCAGATGGTGGGGACATCGGCTTTGGGGTTTTCCTG
AAGACCAAGATGGGGGAGCAGCAGAGTGCTAGGGAGATGACGGAGGTGCTGCCCAGCCAG
CGCTACAATGCCCACATGGTGCCTGAGGATGGGAGCCTCACCTGCCTCCAGGCTGGCGTC
TATGTCCTGCGCTTCGACAACACCTACAGCCGGATGCATGCCAAGAAGCTCAGCTACACT
GTGGAGGTGCTGCTTCCCGACAAGGCCTCTGAGGAGACGCTGCAGAGTCTCAAGGCGATG
AGACCCTCCCCAACACAGTGA
Target 1 GenBank Gene ID
Target 1 GeneCard ID SEC14L4 Link Image
Target 1 GenAtlas ID SEC14L4 Link Image
Target 1 HGNC ID HGNC:20627 Link Image
Target 1 Chromosome Location 22
Target 1 Locus 22q12.2
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Dunham I, Shimizu N, Roe BA, Chissoe S, Hunt AR, Collins JE, Bruskiewich R, Beare DM, Clamp M, Smink LJ, Ainscough R, Almeida JP, Babbage A, Bagguley C, Bailey J, Barlow K, Bates KN, Beasley O, Bird CP, Blakey S, Bridgeman AM, Buck D, Burgess J, Burrill WD, O'Brien KP, et al.: The DNA sequence of human chromosome 22. Nature. 1999 Dec 2;402(6761):489-95. [PubMed Link Image]
  2. Kempna P, Zingg JM, Ricciarelli R, Hierl M, Saxena S, Azzi A: Cloning of novel human SEC14p-like proteins: ligand binding and functional properties. Free Radic Biol Med. 2003 Jun 1;34(11):1458-72. [PubMed Link Image]
Target 1 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 275
Target 2 Name Arachidonate 5-lipoxygenase
Target 2 Synonyms
  1. 5-LO
  2. 5-lipoxygenase
  3. EC 1.13.11.34
Target 2 Gene Name ALOX5
Target 2 Protein Sequence >Arachidonate 5-lipoxygenase 
PSYTVTVATGSQWFAGTDDYIYLSLVGSAGCSEKHLLDKPFYNDFERGAVDSYDVTVDEE
LGEIQLVRIEKRKYWLNDDWYLKYITLKTPHGDYIEFPCYRWITGDVEVVLRDGRAKLAR
DDQIHILKQHRRKELETRQKQYRWMEWNPGFPLSIDAKCHKDLPRDIQFDSEKGVDFVLN
YSKAMENLFINRFMHMFQSSWNDFADFEKIFVKISNTISERVMNHWQEDLMFGYQFLNGC
NPVLIRRCTELPEKLPVTTEMVECSLERQLSLEQEVQQGNIFIVDFELLDGIDANKTDPC
TLQFLAAPICLLYKNLANKIVPIAIQLNQIPGDENPIFLPSDAKYDWLLAKIWVRSSDFH
VHQTITHLLRTHLVSEVFGIAMYRQLPAVHPIFKLLVAHVRFTIAINTKAREQLICECGL
FDKANATGGGGHVQMVQRAMKDLTYASLCFPEAIKARGMESKEDIPYYFYRDDGLLVWEA
IRTFTAEVVDIYYEGDQVVEEDPELQDFVNDVYVYGMRGRKSSGFPKSVKSREQLSEYLT
VVIFTASAQHAAVNFGQYDWCSWIPNAPPTMRAPPPTAKGVVTIEQIVDTLPDRGRSCWH
LGAVWALSQFQENELFLGMYPEEHFIEKPVKEAMARFRKNLEAIVSVIAERNKKKQLPYY
YLSPDRIPNSVAI
Target 2 Number of Residues 684
Target 2 Molecular Weight 77853
Target 2 Theoretical pI 5.54
Target 2 GO Classification
Function
catalytic activity
oxidoreductase activity
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygen
lipoxygenase activity
binding
ion binding
cation binding
transition metal ion binding
iron ion binding
Process
organic acid metabolism
carboxylic acid metabolism
fatty acid metabolism
icosanoid metabolism
leukotriene metabolism
physiological process
metabolism
cellular metabolism
generation of precursor metabolites and energy
electron transport
Component
Not Available
Target 2 General Function Involved in oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygen
Target 2 Specific Function Not Available
Target 2 Pathways
Name SMPDB Link KEGG Link
Prostaglandin and leukotriene metabolism map00590 Link Image
Target 2 Reactions
  • arachidonate + O2 = (6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyicosa-6,8,11,14-tetraenoate
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • None
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 187193 Link Image
Target 2 UniProtKB/Swiss-Prot ID P09917 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name LOX5_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location
  • Cytoplasm
Target 2 Gene Sequence >2025 bp 
ATGCCCTCCTACACGGTCACCGTGGCCACTGGCAGCCAGTGGTTCGCCGGCACTGACGAC
TACATCTACCTCAGCCTCGTGGGCTCGGCGGGCTGCAGCGAGAAGCACCTGCTGGACAAG
CCCTTCTACAACGACTTCGAGCGTGGCGCGGTGGATTCATACGACGTGACTGTGGACGAG
GAACTGGGCGAGATCCAGCTGGTCAGAATCGAGAAGCGCAAGTACTGGCTGAATGACGAC
TGGTACCTGAAGTACATCACGCTGAAGACGCCCCACGGGGACTACATCGAGTTCCCCTGC
TACCGCTGGATCACCGGCGATGTCGAGGTTGTCCTGAGGGATGGACGCGCAAAGTTGGCC
CGAGATGACCAAATTCACATTCTCAAGCAACACCGACGTAAAGAACTGGAAACACGGCAA
AAACAATATCGATGGATGGAGTGGAACCCTGGCTTCCCCTTGAGCATCGATGCCAAATGC
CACAAGGATTTACCCCGTGATATCCAGTTTGATAGTGAAAAAGGAGTGGACTTTGTTCTG
AATTACTCCAAAGCGATGGAGAACCTGTTCATCAACCGCTTCATGCACATGTTCCAGTCT
TCTTGGAATGACTTCGCCGACTTTGAGAAAATCTTTGTCAAGATCAGCAACACTATTTCT
GAGCGGGTCATGAATCACTGGCAGGAAGACCTGATGTTTGGCTACCAGTTCCTGAATGGC
TGCAACCCTGTGTTGATCCGGCGCTGCACAGAGCTGCCCGAGAAGCTCCCGGTGACCACG
GAGATGGTAGAGTGCAGCCTGGAGCGGCAGCTCAGCTTGGAGCAGGAGGTCCAGCAAGGG
AACATTTTCATCGTGGACTTTGAGCTGCTGGATGGCATCGATGCCAACAAAACAGACCCC
TGCACACTCCAGTTCCTGGCCGCTCCCATCTGCTTGCTGTATAAGAACCTGGCCAACAAG
ATTGTCCCCATTGCCATCCAGCTCAACCAAATCCCGGGAGATGAGAACCCTATTTTCCTC
CCTTCGGATGCAAAATACGACTGGCTTTTGGCCAAAATCTGGGTGCGTTCCAGTGACTTC
CACGTCCACCAGACCATCACCCACCTTCTGCGAACACATCTGGTGTCTGAGGTTTTTGGC
ATTGCAATGTACCGCCAGCTGCCTGCTGTGCACCCCATTTTCAAGCTGCTGGTGGCACAC
GTGAGATTCACCATTGCAATCAACACCAAGGCCCGTGAGCAGCTCATCTGCGAGTGTGGC
CTCTTTGACAAGGCCAACGCCACAGGGGGCGGTGGGCACGTGCAGATGGTGCAGAGGGCC
ATGAAGGACCTGACCTATGCCTCCCTGTGCTTTCCCGAGGCCATCAAGGCCCGGGGCATG
GAGAGCAAAGAAGACATCCCCTACTACTTCTACCGGGACGACGGGCTCCTGGTGTGGGAA
GCCATCAGGACGTTCACGGCCGAGGTGGTAGACATCTACTACGAGGGCGACCAGGTGGTG
GAGGAGGACCCGGAGCTGCAGGACTTCGTGAACGATGTCTACGTGTACGGCATGCGGGGC
CGCAAGTCCTCAGGCTTCCCCAAGTCGGTCAAGAGCCGGGAGCAGCTGTCGGAGTACCTG
ACCGTGGTGATCTTCACCGCCTCCGCCCAGCACGCCGCGGTCAACTTCGGCCAGTACGAC
TGGTGCTCCTGGATCCCCAATGCGCCCCCAACCATGCGAGCCCCGCCACCGACTGCCAAG
GGCGTGGTGACCATTGAGCAGATCGTGGACACGCTGCCCGACCGCGGCCGCTCCTGCTGG
CATCTGGGTGCAGTGTGGGCGCTGAGCCAGTTCCAGGAAAACGAGCTGTTCCTGGGCATG
TACCCAGAAGAGCATTTTATCGAGAAGCCTGTGAAGGAAGCCATGGCCCGATTCCGCAAG
AACCTCGAGGCCATTGTCAGCGTGATTGCTGAGCGCAACAAGAAGAAGCAGCTGCCATAT
TACTACTTGTCCCCAGACCGGATTCCGAACAGTGTGGCCATCTGA
Target 2 GenBank Gene ID
Target 2 GeneCard ID ALOX5 Link Image
Target 2 GenAtlas ID ALOX5 Link Image
Target 2 HGNC ID HGNC:435 Link Image
Target 2 Chromosome Location 10
Target 2 Locus 10q11.2
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Werz O, Szellas D, Steinhilber D, Radmark O: Arachidonic acid promotes phosphorylation of 5-lipoxygenase at Ser-271 by MAPK-activated protein kinase 2 (MK2). J Biol Chem. 2002 Apr 26;277(17):14793-800. Epub 2002 Feb 13. [PubMed Link Image]
  2. Ishii S, Noguchi M, Miyano M, Matsumoto T, Noma M: Mutagenesis studies on the amino acid residues involved in the iron-binding and the activity of human 5-lipoxygenase. Biochem Biophys Res Commun. 1992 Feb 14;182(3):1482-90. [PubMed Link Image]
  3. Nguyen T, Falgueyret JP, Abramovitz M, Riendeau D: Evaluation of the role of conserved His and Met residues among lipoxygenases by site-directed mutagenesis of recombinant human 5-lipoxygenase. J Biol Chem. 1991 Nov 15;266(32):22057-62. [PubMed Link Image]
  4. Hoshiko S, Radmark O, Samuelsson B: Characterization of the human 5-lipoxygenase gene promoter. Proc Natl Acad Sci U S A. 1990 Dec;87(23):9073-7. [PubMed Link Image]
  5. Matsumoto T, Funk CD, Radmark O, Hoog JO, Jornvall H, Samuelsson B: Molecular cloning and amino acid sequence of human 5-lipoxygenase. Adv Prostaglandin Thromboxane Leukot Res. 1989;19:466-9. [PubMed Link Image]
  6. Funk CD, Hoshiko S, Matsumoto T, Rdmark O, Samuelsson B: Characterization of the human 5-lipoxygenase gene. Proc Natl Acad Sci U S A. 1989 Apr;86(8):2587-91. [PubMed Link Image]
  7. Matsumoto T, Funk CD, Radmark O, Hoog JO, Jornvall H, Samuelsson B: Molecular cloning and amino acid sequence of human 5-lipoxygenase. Proc Natl Acad Sci U S A. 1988 Jan;85(1):26-30. [PubMed Link Image]
  8. Dixon RA, Jones RE, Diehl RE, Bennett CD, Kargman S, Rouzer CA: Cloning of the cDNA for human 5-lipoxygenase. Proc Natl Acad Sci U S A. 1988 Jan;85(2):416-20. [PubMed Link Image]
Target 2 Drug References
  1. Taccone-Gallucci M, Manca-di-Villahermosa S, Battistini L, Stuffler RG, Tedesco M, Maccarrone M: N-3 PUFAs reduce oxidative stress in ESRD patients on maintenance HD by inhibiting 5-lipoxygenase activity. Kidney Int. 2006 Apr;69(8):1450-4. [PubMed Link Image]
Drug Target 3 [top]
Target 3 ID 283
Target 3 Name SEC14-like protein 2
Target 3 Synonyms
  1. Alpha-tocopherol-associated protein
  2. SPF
  3. Squalene transfer protein
  4. Supernatant protein factor
  5. TAP
  6. hTAP
Target 3 Gene Name SEC14L2
Target 3 Protein Sequence >SEC14-like protein 2 
MSGRVGDLSPRQKEALAKFRENVQDVLPALPNPDDYFLLRWLRARSFDLQKSEAMLRKHV
EFRKQKDIDNIISWQPPEVIQQYLSGGMCGYDLDGCPVWYDIIGPLDAKGLLFSASKQDL
LRTKMRECELLLQECAHQTTKLGRKVETITIIYDCEGLGLKHLWKPAVEAYGEFLCMFEE
NYPETLKRLFVVKAPKLFPVAYNLIKPFLSEDTRKKIMVLGANWKEVLLKHISPDQVPVE
YGGTMTDPDGNPKCKSKINYGGDIPRKYYVRDQVKQQYEHSVQISRGSSHQVEYEILFPG
CVLRWQFMSDGADVGFGIFLKTKMGERQRAGEMTEVLPNQRYNSHLVPEDGTLTCSDPGI
YVLRFDNTYSFIHAKKVNFTVEVLLPDKASEEKMKQLGAGTPK
Target 3 Number of Residues 409
Target 3 Molecular Weight 46146
Target 3 Theoretical pI 7.94
Target 3 GO Classification
Function
carrier activity
protein carrier activity
transporter activity
Process
protein transport
intracellular protein transport
physiological process
cellular physiological process
transport
Component
membrane
cell
intracellular
Target 3 General Function Involved in transporter activity
Target 3 Specific Function Carrier protein. Binds to some hydrophobic molecules and promotes their transfer between the different cellular sites. Binds with high affinity to alpha-tocopherol. Also binds with a weaker affinity to other tocopherols and to tocotrienols. May have a transcriptional activatory activity via its association with alpha-tocopherol. Probably recognizes and binds some squalene structure, suggesting that it may regulate cholesterol biosynthesis by increasing the transfer of squalene to a metabolic active pool in the cell
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • None
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 5596693 Link Image
Target 3 UniProtKB/Swiss-Prot ID O76054 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name S14L2_HUMAN Link Image
Target 3 PDB ID 1OLM Link Image
Target 3 PDB File Show
Target 3 3D Structure
Target 3 Cellular Location
  • Cytoplasm. Nucleus. Cytoplasmic in absence of alpha-tocopherol, and nuclear in presence of alpha-toc
Target 3 Gene Sequence >1212 bp 
ATGAGCGGCAGAGTCGGCGATCTGAGCCCCAGGCAGAAGGAGGCATTGGCCAAGTTTCGG
GAGAATGTCCAGGATGTGCTGCCGGCCCTGCCGAATCCAGATGACTATTTTCTCCTGCGT
TGGCTCCGAGCCAGAAGCTTCGACCTGCAGAAGTCGGAGGCCATGCTCCGGAAGCATGTG
GAGTTCCGAAAGCAAAAGGACATTGACAACATCATTAGCTGGCAGCCTCCAGAGGTGATC
CAACAGTATCTGTCAGGGGGTATGTGTGGCTATGACCTGGATGGCTGCCCAGTCTGGTAC
GACATAATTGGACCTCTGGATGCCAAGGGTCTGCTGTTCTCAGCCTCCAAACAGGACCTG
CTGAGGACCAAGATGCGGGAGTGTGAGCTGCTTCTGCAAGAGTGTGCCCACCAGACCACA
AAGTTGGGGAGGAAGGTGGAGACCATCACCATAATTTATGACTGCGAGGGGCTTGGCCTC
AAGCATCTCTGGAAGCCTGCTGTGGAGGCCTATGGAGAGTTTCTCTGCATGTTTGAGGAA
AATTATCCCGAAACACTGAAGCGTCTTTTTGTTGTTAAAGCCCCCAAACTGTTTCCTGTG
GCCTATAACCTCATCAAACCCTTCCTGAGTGAGGACACTCGTAAGAAGATCATGGTCCTG
GGAGCAAATTGGAAGGAGGTTTTACTGAAACATATCAGCCCTGACCAGGTGCCTGTGGAG
TATGGGGGCACCATGACTGACCCTGATGGAAACCCCAAGTGCAAATCCAAGATCAACTAC
GGGGGTGACATCCCCAGGAAGTATTATGTGCGAGACCAGGTGAAACAGCAGTATGAACAC
AGCGTGCAGATTTCCCGTGGCTCCTCCCACCAAGTGGAGTATGAGATCCTCTTCCCTGGC
TGTGTCCTCAGGTGGCAGTTTATGTCAGATGGAGCGGATGTTGGTTTTGGGATTTTCCTG
AAGACCAAGATGGGAGAGAGGCAGCGGGCAGGGGAGATGACAGAGGTGCTGCCCAACCAG
AGGTACAACTCCCACCTGGTCCCTGAAGATGGGACCCTCACCTGCAGTGATCCTGGCATC
TATGTCCTGCGGTTTGACAACACCTACAGCTTCATTCATGCCAAGAAGGTCAATTTCACT
GTGGAGGTCCTGCTTCCAGACAAAGCCTCAGAAGAGAAGATGAAACAGCTGGGGGCAGGC
ACCCCGAAATAA
Target 3 GenBank Gene ID
Target 3 GeneCard ID SEC14L2 Link Image
Target 3 GenAtlas ID SEC14L2 Link Image
Target 3 HGNC ID HGNC:10699 Link Image
Target 3 Chromosome Location 22
Target 3 Locus 22q12.2
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Hirosawa M, Nagase T, Ishikawa K, Kikuno R, Nomura N, Ohara O: Characterization of cDNA clones selected by the GeneMark analysis from size-fractionated cDNA libraries from human brain. DNA Res. 1999 Oct 29;6(5):329-36. [PubMed Link Image]
  2. Dunham I, Shimizu N, Roe BA, Chissoe S, Hunt AR, Collins JE, Bruskiewich R, Beare DM, Clamp M, Smink LJ, Ainscough R, Almeida JP, Babbage A, Bagguley C, Bailey J, Barlow K, Bates KN, Beasley O, Bird CP, Blakey S, Bridgeman AM, Buck D, Burgess J, Burrill WD, O'Brien KP, et al.: The DNA sequence of human chromosome 22. Nature. 1999 Dec 2;402(6761):489-95. [PubMed Link Image]
  3. Zimmer S, Stocker A, Sarbolouki MN, Spycher SE, Sassoon J, Azzi A: A novel human tocopherol-associated protein: cloning, in vitro expression, and characterization. J Biol Chem. 2000 Aug 18;275(33):25672-80. [PubMed Link Image]
  4. Yamauchi J, Iwamoto T, Kida S, Masushige S, Yamada K, Esashi T: Tocopherol-associated protein is a ligand-dependent transcriptional activator. Biochem Biophys Res Commun. 2001 Jul 13;285(2):295-9. [PubMed Link Image]
Target 3 Drug References
  1. Neuzil J, Dong LF, Wang XF, Zingg JM: Tocopherol-associated protein-1 accelerates apoptosis induced by alpha-tocopheryl succinate in mesothelioma cells. Biochem Biophys Res Commun. 2006 May 19;343(4):1113-7. Epub 2006 Mar 31. [PubMed Link Image]
  2. Ni J, Pang ST, Yeh S: Differential retention of alpha-vitamin E is correlated with its transporter gene expression and growth inhibition efficacy in prostate cancer cells. Prostate. 2007 Apr 1;67(5):463-71. [PubMed Link Image]
Drug Target 4 [top]
Target 4 ID 375
Target 4 Name SEC14-like protein 3
Target 4 Synonyms
  1. Tocopherol-associated protein 2
Target 4 Gene Name SEC14L3
Target 4 Protein Sequence >SEC14-like protein 3 
MSGRVGDLSPKQAETLAKFRENVQDVLPALPNPDDYFLLRWLRARNFDLQKSEALLRKYM
EFRKTMDIDHILDWQPPEVIQKYMPGGLCGYDRDGCPVWYDIIGPLDPKGLLFSVTKQDL
LKTKMRDCERILHECDLQTERLGKKIETIVMIFDCEGLGLKHFWKPLVEVYQEFFGLLEE
NYPETLKFMLIVKATKLFPVGYNLMKPFLSEDTRRKIIVLGNNWKEGLLKLISPEELPAQ
FGGTLTDPDGNPKCLTKINYGGEIPKSMYVRDQVKTQYEHSVQINRGSSHQVEYEILFPG
CVLRWQFSSDGADIGFGVFLKTKMGERQRAGEMTDVLPSQRYNAHMVPEDGNLTCSEAGV
YVLRFDNTYSFVHAKKVSFTVEVLLPDEGMQKYDKELTPV
Target 4 Number of Residues 406
Target 4 Molecular Weight 46049
Target 4 Theoretical pI 5.97
Target 4 GO Classification
Function
carrier activity
protein carrier activity
transporter activity
Process
protein transport
intracellular protein transport
physiological process
cellular physiological process
transport
Component
membrane
cell
intracellular
Target 4 General Function Involved in transporter activity
Target 4 Specific Function Probable hydrophobic ligand-binding protein; may play a role in the transport of hydrophobic ligands like tocopherol, squalene and phospholipids
Target 4 Pathways Not Available
Target 4 Reactions Not Available
Target 4 Pfam Domain Function
Target 4 Signals
  • None
Target 4 Transmembrane Regions
  • None
Target 4 Essentiality Non-Essential
Target 4 GenBank ID Protein 27803382 Link Image
Target 4 UniProtKB/Swiss-Prot ID Q9UDX4 Link Image
Target 4 UniProtKB/Swiss-Prot Entry Name S14L3_HUMAN Link Image
Target 4 PDB ID Not Available
Target 4 Cellular Location Not Available
Target 4 Gene Sequence >1203 bp 
ATGAGCGGCCGAGTTGGAGACCTGAGCCCCAAACAGGCAGAGACCCTGGCCAAGTTCCGA
GAAAACGTCCAGGATGTGCTTCCTGCCCTGCCCAACCCTGATGATTATTTCCTTCTACGC
TGGCTCCGAGCTCGGAATTTTGACTTGCAGAAGTCGGAGGCTTTGCTCCGCAAGTACATG
GAGTTCCGGAAGACCATGGATATTGACCATATCCTTGATTGGCAGCCCCCAGAGGTGATC
CAGAAGTACATGCCTGGGGGCCTGTGTGGCTATGACCGTGATGGCTGCCCCGTGTGGTAT
GACATCATTGGGCCACTTGATCCCAAGGGGTTGCTCTTCTCAGTCACCAAGCAGGACCTG
CTCAAGACCAAGATGAGGGACTGTGAGCGCATCCTGCATGAGTGTGACCTGCAGACAGAG
AGGCTAGGGAAGAAGATTGAGACCATCGTGATGATATTTGACTGTGAGGGCCTGGGACTG
AAACACTTCTGGAAACCTCTGGTAGAAGTGTACCAGGAGTTCTTTGGCCTCCTTGAAGAG
AATTACCCAGAGACCCTGAAGTTCATGCTCATCGTGAAAGCTACCAAACTGTTCCCTGTG
GGCTACAACCTCATGAAGCCATTCCTGAGTGAGGACACTCGCAGGAAAATTATTGTGTTG
GGAAATAACTGGAAGGAAGGTTTGCTGAAACTCATCAGTCCTGAGGAACTGCCTGCCCAG
TTTGGGGGCACCCTGACTGACCCAGATGGGAACCCCAAATGTTTAACCAAGATTAACTAT
GGCGGGGAGATCCCCAAGTCCATGTACGTGCGGGACCAGGTGAAGACTCAGTACGAGCAC
TCGGTGCAGATCAACCGCGGCTCATCACACCAAGTGGAATACGAGATCCTATTTCCAGGC
TGCGTTCTCAGGTGGCAGTTCTCATCTGATGGTGCGGACATCGGCTTCGGAGTTTTCCTG
AAGACCAAGATGGGGGAGCGACAGCGGGCAGGGGAGATGACAGATGTTCTACCCAGCCAG
CGCTATAACGCCCACATGGTGCCCGAGGATGGGAACCTCACCTGCTCAGAGGCCGGCGTC
TATGTCCTACGCTTCGACAACACCTATAGCTTTGTCCACGCCAAGAAGGTCAGCTTCACA
GTGGAGGTCCTGCTCCCTGACGAGGGCATGCAGAAATATGATAAGGAGCTCACCCCTGTC
TAG
Target 4 GenBank Gene ID
Target 4 GeneCard ID SEC14L3 Link Image
Target 4 GenAtlas ID SEC14L3 Link Image
Target 4 HGNC ID HGNC:18655 Link Image
Target 4 Chromosome Location 22
Target 4 Locus 22q12.2
Target 4 SNPs SNPJam Report Link Image
Target 4 General References
  1. Dunham I, Shimizu N, Roe BA, Chissoe S, Hunt AR, Collins JE, Bruskiewich R, Beare DM, Clamp M, Smink LJ, Ainscough R, Almeida JP, Babbage A, Bagguley C, Bailey J, Barlow K, Bates KN, Beasley O, Bird CP, Blakey S, Bridgeman AM, Buck D, Burgess J, Burrill WD, O'Brien KP, et al.: The DNA sequence of human chromosome 22. Nature. 1999 Dec 2;402(6761):489-95. [PubMed Link Image]
  2. Kempna P, Zingg JM, Ricciarelli R, Hierl M, Saxena S, Azzi A: Cloning of novel human SEC14p-like proteins: ligand binding and functional properties. Free Radic Biol Med. 2003 Jun 1;34(11):1458-72. [PubMed Link Image]
Target 4 Drug References
  1. Ye X, Ji C, Yin G, Tang R, Zeng L, Gu S, Ying K, Xie Y, Zhao RC, Mao Y: Characterization of a human Sec14-like protein cDNA SEC14L3 highly homologous to human SPF/TAP. Mol Biol Rep. 2004 Mar;31(1):59-63. [PubMed Link Image]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  3. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 5 [top]
Target 5 ID 708
Target 5 Name Alpha-tocopherol transfer protein
Target 5 Synonyms
  1. Alpha-TTP
Target 5 Gene Name TTPA
Target 5 Protein Sequence >Alpha-tocopherol transfer protein 
MAEARSQPSAGPQLNALPDHSPLLQPGLAALRRRAREAGVPLAPLPLTDSFLLRFLRARD
FDLDLAWRLLKNYYKWRAECPEISADLHPRSIIGLLKAGYHGVLRSRDPTGSKVLIYRIA
HWDPKVFTAYDVFRVSLITSELIVQEVETQRNGIKAIFDLEGWQFSHAFQITPSVAKKIA
AVLTDSFPLKVRGIHLINEPVIFHAVFSMIKPFLTEKIKERIHMHGNNYKQSLLQHFPDI
LPLEYGGEEFSMEDICQEWTNFIMKSEDYLSSISESIQ
Target 5 Number of Residues 282
Target 5 Molecular Weight 31750
Target 5 Theoretical pI 7.78
Target 5 GO Classification
Function
transporter activity
Process
physiological process
cellular physiological process
transport
Component
cell
intracellular
Target 5 General Function Involved in vitamin E transporter activity
Target 5 Specific Function Binds alpha-tocopherol and enhances its transfer between separate membranes
Target 5 Pathways Not Available
Target 5 Reactions Not Available
Target 5 Pfam Domain Function
Target 5 Signals
  • None
Target 5 Transmembrane Regions
  • None
Target 5 Essentiality Non-Essential
Target 5 GenBank ID Protein 699601 Link Image
Target 5 UniProtKB/Swiss-Prot ID P49638 Link Image
Target 5 UniProtKB/Swiss-Prot Entry Name TTPA_HUMAN Link Image
Target 5 PDB ID 1OIZ Link Image
Target 5 PDB File Show
Target 5 3D Structure
Target 5 Cellular Location
  • Cytoplasm
Target 5 Gene Sequence >837 bp 
ATGGCAGAGGCGCGATCCCAGCCCTCGGCGGGGCCGCAGCTCAACGCGCTACCGGACCAC
TCTCCGTTGCTGCAGCCGGGCCTGGCGGCGCTGCGGCGCCGGGCCCGGGAAGCTGGCGTC
CCGCTCGCGCCGCTGCCGCTCACCGACTCCTTCCTGCTGCGGTTCCTGCGCGCCCGGGAT
TTCGATCTGGACCTGGCCTGGCGGTTACTAAAAAACTATTATAAGTGGAGAGCAGAATGT
CCAGAAATAAGTGCAGATCTACACCCTAGAAGTATTATTGGCCTCCTAAAGGCTGGCTAC
CATGGAGTCCTGAGATCCAGGGATCCCACTGGCAGCAAAGTTCTTATTTACAGAATCGCA
CACTGGGACCCCAAAGTTTTTACAGCTTATGACGTATTTCGAGTAAGTCTAATCACATCC
GAGCTTATTGTACAGGAGGTAGAAACTCAGCGGAATGGAATCAAGGCTATCTTTGATCTG
GAAGGTTGGCAGTTTTCTCATGCTTTTCAAATCACTCCATCCGTAGCCAAGAAGATTGCT
GCTGTACTTACGGATTCATTTCCATTGAAAGTTCGTGGCATCCATTTGATAAATGAACCA
GTAATTTTCCATGCTGTCTTTTCCATGATCAAACCATTCCTGACTGAAAAAATTAAGGAA
CGGATTCACATGCATGGGAACAACTACAAACAAAGCTTGCTTCAGCATTTCCCAGACATT
CTTCCTCTGGAATATGGTGGTGAAGAATTCTCCATGGAGGACATTTGTCAGGAATGGACA
AATTTTATAATGAAGTCTGAAGATTATCTCAGCAGCATTTCTGAGAGCATTCAATGA
Target 5 GenBank Gene ID
Target 5 GeneCard ID TTPA Link Image
Target 5 GenAtlas ID TTPA Link Image
Target 5 HGNC ID HGNC:12404 Link Image
Target 5 Chromosome Location 8
Target 5 Locus 8q13.1-q13.3
Target 5 SNPs SNPJam Report Link Image
Target 5 General References
  1. Gotoda T, Arita M, Arai H, Inoue K, Yokota T, Fukuo Y, Yazaki Y, Yamada N: Adult-onset spinocerebellar dysfunction caused by a mutation in the gene for the alpha-tocopherol-transfer protein. N Engl J Med. 1995 Nov 16;333(20):1313-8. [PubMed Link Image]
  2. Arita M, Sato Y, Miyata A, Tanabe T, Takahashi E, Kayden HJ, Arai H, Inoue K: Human alpha-tocopherol transfer protein: cDNA cloning, expression and chromosomal localization. Biochem J. 1995 Mar 1;306 ( Pt 2):437-43. [PubMed Link Image]
  3. Hentati A, Deng HX, Hung WY, Nayer M, Ahmed MS, He X, Tim R, Stumpf DA, Siddique T, Ahmed: Human alpha-tocopherol transfer protein: gene structure and mutations in familial vitamin E deficiency. Ann Neurol. 1996 Mar;39(3):295-300. [PubMed Link Image]
Target 5 Drug References Not Available
Drug Target 6 [top]
Target 6 ID 997
Target 6 Name Protein kinase C beta type
Target 6 Synonyms
  1. EC 2.7.11.13
  2. PKC-B
  3. PKC-beta
Target 6 Gene Name PRKCB1
Target 6 Protein Sequence >Protein kinase C beta type 
MADPAAGPPPSEGEESTVRFARKGALRQKNVHEVKNHKFTARFFKQPTFCSHCTDFIWGF
GKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPASDDPRSKHKFKIHTYSSPTFCDHCGS
LLYGLIHQGMKCDTCMMNVHKRCVMNVPSLCGTDHTERRGRIYIQAHIDRDVLIVLVRDA
KNLVPMDPNGLSDPYVKLKLIPDPKSESKQKTKTIKCSLNPEWNETFRFQLKESDKDRRL
SVEIWDWDLTSRNDFMGSLSFGISELQKASVDGWFKLLSQEEGEYFNVPVPPEGSEANEE
LRQKFERAKISQGTKVPEEKTTNTVSKFDNNGNRDRMKLTDFNFLMVLGKGSFGKVMLSE
RKGTDELYAVKILKKDVVIQDDDVECTMVEKRVLALPGKPPFLTQLHSCFQTMDRLYFVM
EYVNGGDLMYHIQQVGRFKEPHAVFYAAEIAIGLFFLQSKGIIYRDLKLDNVMLDSEGHI
KIADFGMCKENIWDGVTTKTFCGTPDYIAPEIIAYQPYGKSVDWWAFGVLLYEMLAGQAP
FEGEDEDELFQSIMEHNVAYPKSMSKEAVAICKGLMTKHPGKRLGCGPEGERDIKEHAFF
RYIDWEKLERKEIQPPYKPKARDKRDTSNFDKEFTRQPVELTPTDKLFIMNLDQNEFAGF
SYTNPEFVINV
Target 6 Number of Residues 682
Target 6 Molecular Weight 76870
Target 6 Theoretical pI 7.00
Target 6 GO Classification
Function
binding
nucleotide binding
purine nucleotide binding
adenyl nucleotide binding
ATP binding
catalytic activity
transferase activity
transferase activity, transferring phosphorus-containing groups
kinase activity
protein kinase activity
protein serine/threonine kinase activity
Process
physiological process
metabolism
macromolecule metabolism
biopolymer metabolism
biopolymer modification
protein modification
protein amino acid phosphorylation
cellular process
cell communication
signal transduction
intracellular signaling cascade
Component
Not Available
Target 6 General Function Involved in protein serine/threonine kinase activity
Target 6 Specific Function This is a calcium-activated, phospholipid-dependent, serine- and threonine-specific enzyme. PKC is activated by diacylglycerol which in turn phosphorylates a range of cellular proteins. PKC also serves as the receptor for phorbol esters, a class of tumor promoters. May be considered as a novel component of the NF-kappa-B signaling axis responsible for the survival and activation of B-cells after BCR cross-linking
Target 6 Pathways Not Available
Target 6 Reactions
  • ATP + a protein = ADP + a phosphoprotein
Target 6 Pfam Domain Function
Target 6 Signals
  • None
Target 6 Transmembrane Regions
  • None
Target 6 Essentiality Non-Essential
Target 6 GenBank ID Protein 189969 Link Image
Target 6 UniProtKB/Swiss-Prot ID P05771 Link Image
Target 6 UniProtKB/Swiss-Prot Entry Name KPCB_HUMAN Link Image
Target 6 PDB ID Not Available
Target 6 Cellular Location
  • Cytoplasm. Membrane
  • peripheral membrane protein (By similarity)
Target 6 Gene Sequence >2022 bp 
ATGGCTGACCCGGCTGCGGGGCCGCCGCCGAGCGAGGGCGAGGAGAGCACCGTGCGCTTC
GCCCGCAAAGGCGCCCTCAGGCAGAAGAACGTGCATGAGGTCAAGAACCACAAATTCACC
GCCCGCTTCTTCAAGCAGCCCACCTTCTGCAGCCACTGCACCGACTTCATCTGGGGCTTC
GGGAAGCAGGGATTCCAGTGCCAAGTTTGCTGCTTTGTGGTGCACAAGCGGTGCCATGAA
TTTGTCACATTCTCCTGCCCTGGCGCTGACAAGGGTCCAGCCTCCGATGACCCCCGCAGC
AAACACAAGTTTAAGATCCACACGTACTCCAGCCCCACGTTTTGTGACCACTGTGGGTCA
CTGCTGTATGGACTCATCCACCAGGGGATGAAATGTGACACCTGCATGATGAACGTGCAC
AAGCGCTGCGTGATGAATGTTCCCAGCCTGTGTGGCACGGACCACACGGAGCGCCGCGGC
CGCATCTACATCCAGGCCCACATCGACAGGGACGTCCTCATTGTCCTCGTAAGAGATGCT
AAAAACCTTGTACCTATGGACCCCAATGGCCTGTCAGATCCCTACGTAAAACTGAAACTG
ATTCCCGATCCCAAAAGTGAGAGCAAACAGAAGACCAAAACCATCAAATGCTCCCTCAAC
CCTGAGTGGAATGAGACATTTAGATTTCAGCTGAAAGAATCGGACAAAGACAGAAGACTG
TCAGTAGAGATTTGGGATTGGGATTTGACCAGCAGGAATGACTTCATGGGATCTTTGTCC
TTTGGGATTTCTGAACTTCAGAAAGCCAGTGTTGATGGCTGGTTTAAGTTACTGAGCCAG
GAGGAAGGCGAGTACTTCAATGTGCCTGTGCCACCAGAAGGAAGTGAGGCCAATGAAGAA
CTGCGGCAGAAATTTGAGAGGGCCAAGATCAGTCAGGGAACCAAGGTCCCGGAAGAAAAG
ACGACCAACACTGTCTCCAAATTTGACAACAATGGCAACAGAGACCGGATGAAACTGACC
GATTTTAACTTCCTAATGGTGCTGGGGAAAGGCAGCTTTGGCAAGGTCATGCTTTCAGAA
CGAAAAGGCACAGATGAGCTCTATGCTGTGAAGATCCTGAAGAAGGACGTTGTGATCCAA
GATGATGACGTGGAGTGCACTATGGTGGAGAAGCGGGTGTTGGCCCTGCCCGGGAAGCCG
CCCTTCCTGACCCAGCTCCACTCCTGCTTCCAGACCATGGACCGCCTGTACTTTGTGATG
GAGTACGTGAATGGGGGCGACCTCATGTATCACATCCAGCAAGTCGGCCGGTTCAAGGAG
CCCCATGCTGTATTTTACGCTGCAGAAATTGCCATCGGTCTGTTCTTCTTACAGAGTAAG
GGCATCATTTACCGTGACCTAAAACTTGACAACGTGATGCTCGATTCTGAGGGACACATC
AAGATTGCCGATTTTGGCATGTGTAAGGAAAACATCTGGGATGGGGTGACAACCAAGACA
TTCTGTGGCACTCCAGACTACATCGCCCCCGAGATAATTGCTTATCAGCCCTATGGGAAG
TCCGTGGATTGGTGGGCATTTGGAGTCCTGCTGTATGAAATGTTGGCTGGGCAGGCACCC
TTTGAAGGGGAGGATGAGGATGAACTCTTCCAATCCATCATGGAACACAACGTAGCCTAT
CCCAAGTCTATGTCCAAGGAAGCTGTGGCCATCTGCAAAGGGCTGATGACCAAACACCCA
GGCAAACGTCTGGGTTGTGGACCTGAAGGTGAACGTGATATCAAAGAGCATGCATTTTTC
CGGTATATTGATTGGGAGAAACTTGAACGCAAAGAGATTCAGCCCCCTTATAAGCCAAAA
GCTTGTGGGCGAAATGCTGAAAACTTCGACCGATTTTTCACCCGCCATCCACCAGTCCTA
ACACCTCCTGACCAGGAAGTCATCAGGAATATTGACCAATCAGAATTCGAAGGATTTTCC
TTTGTTAACTCTGAATTTTTAAAACCCGAAGTCAAGAGCTAA
Target 6 GenBank Gene ID
Target 6 GeneCard ID PRKCB1 Link Image
Target 6 GenAtlas ID PRKCB1 Link Image
Target 6 HGNC ID HGNC:9395 Link Image
Target 6 Chromosome Location 16
Target 6 Locus 16p11.2
Target 6 SNPs SNPJam Report Link Image
Target 6 General References
  1. Loftus BJ, Kim UJ, Sneddon VP, Kalush F, Brandon R, Fuhrmann J, Mason T, Crosby ML, Barnstead M, Cronin L, Deslattes Mays A, Cao Y, Xu RX, Kang HL, Mitchell S, Eichler EE, Harris PC, Venter JC, Adams MD: Genome duplications and other features in 12 Mb of DNA sequence from human chromosome 16p and 16q. Genomics. 1999 Sep 15;60(3):295-308. [PubMed Link Image]
  2. Gevaert K, Goethals M, Martens L, Van Damme J, Staes A, Thomas GR, Vandekerckhove J: Exploring proteomes and analyzing protein processing by mass spectrometric identification of sorted N-terminal peptides. Nat Biotechnol. 2003 May;21(5):566-9. Epub 2003 Mar 31. [PubMed Link Image]
  3. Obeid LM, Blobe GC, Karolak LA, Hannun YA: Cloning and characterization of the major promoter of the human protein kinase C beta gene. Regulation by phorbol esters. J Biol Chem. 1992 Oct 15;267(29):20804-10. [PubMed Link Image]
  4. Niino YS, Ohno S, Suzuki K: Positive and negative regulation of the transcription of the human protein kinase C beta gene. J Biol Chem. 1992 Mar 25;267(9):6158-63. [PubMed Link Image]
  5. Kubo K, Ohno S, Suzuki K: Nucleotide sequence of the 3' portion of a human gene for protein kinase C beta I/beta II. Nucleic Acids Res. 1987 Sep 11;15(17):7179-80. [PubMed Link Image]
  6. Kubo K, Ohno S, Suzuki K: Primary structures of human protein kinase C beta I and beta II differ only in their C-terminal sequences. FEBS Lett. 1987 Oct 19;223(1):138-42. [PubMed Link Image]
  7. Coussens L, Rhee L, Parker PJ, Ullrich A: Alternative splicing increases the diversity of the human protein kinase C family. DNA. 1987 Oct;6(5):389-94. [PubMed Link Image]
  8. Coussens L, Parker PJ, Rhee L, Yang-Feng TL, Chen E, Waterfield MD, Francke U, Ullrich A: Multiple, distinct forms of bovine and human protein kinase C suggest diversity in cellular signaling pathways. Science. 1986 Aug 22;233(4766):859-66. [PubMed Link Image]
  9. Mahajna J, King P, Parker P, Haley J: Autoregulation of cloned human protein kinase C beta and gamma gene promoters in U937 cells. DNA Cell Biol. 1995 Mar;14(3):213-22. [PubMed Link Image]
Target 6 Drug References
  1. Ganz MB, Seftel A: Glucose-induced changes in protein kinase C and nitric oxide are prevented by vitamin E. Am J Physiol Endocrinol Metab. 2000 Jan;278(1):E146-52. [PubMed Link Image]
  2. Huang Y, Ishizuka T, Miura A, Kajita K, Ishizawa M, Kimura M, Yamamoto Y, Kawai Y, Morita H, Uno Y, Yasuda K: Effect of 1 alpha,25-dihydroxy vitamin D3 and vitamin E on insulin-induced glucose uptake in rat adipocytes. Diabetes Res Clin Pract. 2002 Mar;55(3):175-83. [PubMed Link Image]
  3. Wigg SJ, Tare M, Forbes J, Cooper ME, Thomas MC, Coleman HA, Parkington HC, O'Brien RC: Early vitamin E supplementation attenuates diabetes-associated vascular dysfunction and the rise in protein kinase C-beta in mesenteric artery and ameliorates wall stiffness in femoral artery of Wistar rats. Diabetologia. 2004 Jun;47(6):1038-46. Epub 2004 Jun 8. [PubMed Link Image]
  4. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  5. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 7 [top]
Target 7 ID 1284
Target 7 Name Orphan nuclear receptor PXR
Target 7 Synonyms
  1. Orphan nuclear receptor PAR1
  2. Pregnane X receptor
  3. SXR
  4. Steroid and xenobiotic receptor
Target 7 Gene Name NR1I2
Target 7 Protein Sequence >Orphan nuclear receptor PXR 
MEVRPKESWNHADFVHCEDTESVPGKPSVNADEEVGGPQICRVCGDKATGYHFNVMTCEG
CKGFFRRAMKRNARLRCPFRKGACEITRKTRRQCQACRLRKCLESGMKKEMIMSDEAVEE
RRALIKRKKSERTGTQPLGVQGLTEEQRMMIRELMDAQMKTFDTTFSHFKNFRLPGVLSS
GCELPESLQAPSREEAAKWSQVRKDLCSLKVSLQLRGEDGSVWNYKPPADSGGKEIFSLL
PHMADMSTYMFKGIISFAKVISYFRDLPIEDQISLLKGAAFELCQLRFNTVFNAETGTWE
CGRLSYCLEDTAGGFQQLLLEPMLKFHYMLKKLQLHEEEYVLMQAISLFSPDRPGVLQHR
VVDQLQEQFAITLKSYIECNRPQPAHRFLFLKIMAMLTELRSINAQHTQRLLRIQDIHPF
ATPLMQELFGITGS
Target 7 Number of Residues 441
Target 7 Molecular Weight 49762
Target 7 Theoretical pI 8.44
Target 7 GO Classification
Function
signal transducer activity
receptor activity
ligand-dependent nuclear receptor activity
steroid hormone receptor activity
binding
nucleic acid binding
DNA binding
transcription factor activity
Process
regulation of biological process
regulation of physiological process
regulation of metabolism
regulation of cellular metabolism
regulation of nucleobase, nucleoside, nucleotide and nucleic acid metabolism
regulation of transcription
regulation of transcription, DNA-dependent
Component
organelle
membrane-bound organelle
intracellular membrane-bound organelle
nucleus
Target 7 General Function Involved in transcription factor activity
Target 7 Specific Function Orphan receptor; its natural ligand is probably pregnane. Binds to a response element in the CYP3A4 and ABCB1/MDR1 genes promoter. Activates its expression in response to a wide variety of endobiotics and xenobiotics
Target 7 Pathways Not Available
Target 7 Reactions Not Available
Target 7 Pfam Domain Function
Target 7 Signals
  • None
Target 7 Transmembrane Regions
  • None
Target 7 Essentiality Non-Essential
Target 7 GenBank ID Protein 3511138 Link Image
Target 7 UniProtKB/Swiss-Prot ID O75469 Link Image
Target 7 UniProtKB/Swiss-Prot Entry Name PXR_HUMAN Link Image
Target 7 PDB ID 1NRL Link Image
Target 7 PDB File Show
Target 7 3D Structure
Target 7 Cellular Location
  • Nucleus
Target 7 Gene Sequence >1305 bp 
CTGGAGGTGAGACCCAAAGAAAGCTGGAACCATGCTGACTTTGTACACTGTGAGGACACA
GAGTCTGTTCCTGGAAAGCCCAGTGTCAACGCAGATGAGGAAGTCGGAGGTCCCCAAATC
TGCCGTGTATGTGGGGACAAGGCCACTGGCTATCACTTCAATGTCATGACATGTGAAGGA
TGCAAGGGCTTTTTCAGGAGGGCCATGAAACGCAACGCCCGGCTGAGGTGCCCCTTCCGG
AAGGGCGCCTGCGAGATCACCCGGAAGACCCGGCGACAGTGCCAGGCCTGCCGCCTGCGC
AAGTGCCTGGAGAGCGGCATGAAGAAGGAGATGATCATGTCCGACGAGGCCGTGGAGGAG
AGGCGGGCCTTGATCAAGCGGAAGAAAAGTGAACGGACAGGGACTCAGCCACTGGGAGTG
CAGGGGCTGACAGAGGAGCAGCGGATGATGATCAGGGAGCTGATGGACGCTCAGATGAAA
ACCTTTGACACTACCTTCTCCCATTTCAAGAATTTCCGGCTGCCAGGGGTGCTTAGCAGT
GGCTGCGAGTTGCCAGAGTCTCTGCAGGCCCCATCGAGGGAAGAAGCTGCCAAGTGGAGC
CAGGTCCGGAAAGATCTGTGCTCTTTGAAGGTCTCTCTGCAGCTGCGGGGGGAGGATGGC
AGTGTCTGGAACTACAAACCCCCAGCCGACAGTGGCGGGAAAGAGATCTTCTCCCTGCTG
CCCCACATGGCTGACATGTCAACCTACATGTTCAAAGGCATCATCAGCTTTGCCAAAGTC
ATCTCCTACTTCAGGGACTTGCCCATCGAGGACCAGATCTCCCTGCTGAAGGGGGCCGCT
TTCGAGCTGTGTCAACTGAGATTCAACACAGTGTTCAACGCGGAGACTGGAACCTGGGAG
TGTGGCCGGCTGTCCTACTGCTTGGAAGACACTGCAGGTGGCTTCCAGCAACTTCTACTG
GAGCCCATGCTGAAATTCCACTACATGCTGAAGAAGCTGCAGCTGCATGAGGAGGAGTAT
GTGCTGATGCAGGCCATCTCCCTCTTCTCCCCAGACCGCCCAGGTGTGCTGCAGCACCGC
GTGGTGGACCAGCTGCAGGAGCAATTCGCCATTACTCTGAAGTCCTACATTGAATGCAAT
CGGCCCCAGCCTGCTCATAGGTTCTTGTTCCTGAAGATCATGGCTATGCTCACCGAGCTC
CGCAGCATCAATGCTCAGCACACCCAGCGGCTGCTGCGCATCCAGGACATACACCCCTTT
GCTACGCCCCTCATGCAGGAGTTGTTCGGCATCACAGGTAGCTGA
Target 7 GenBank Gene ID
Target 7 GeneCard ID NR1I2 Link Image
Target 7 GenAtlas ID NR1I2 Link Image
Target 7 HGNC ID HGNC:7968 Link Image
Target 7 Chromosome Location 3
Target 7 Locus 3q12-q13.3
Target 7 SNPs SNPJam Report Link Image
Target 7 General References
  1. Watkins RE, Wisely GB, Moore LB, Collins JL, Lambert MH, Williams SP, Willson TM, Kliewer SA, Redinbo MR: The human nuclear xenobiotic receptor PXR: structural determinants of directed promiscuity. Science. 2001 Jun 22;292(5525):2329-33. Epub 2001 Jun 14. [PubMed Link Image]
  2. Zhang J, Kuehl P, Green ED, Touchman JW, Watkins PB, Daly A, Hall SD, Maurel P, Relling M, Brimer C, Yasuda K, Wrighton SA, Hancock M, Kim RB, Strom S, Thummel K, Russell CG, Hudson JR Jr, Schuetz EG, Boguski MS: The human pregnane X receptor: genomic structure and identification and functional characterization of natural allelic variants. Pharmacogenetics. 2001 Oct;11(7):555-72. [PubMed Link Image]
  3. Kawana K, Ikuta T, Kobayashi Y, Gotoh O, Takeda K, Kawajiri K: Molecular mechanism of nuclear translocation of an orphan nuclear receptor, SXR. Mol Pharmacol. 2003 Mar;63(3):524-31. [PubMed Link Image]
  4. Lehmann JM, McKee DD, Watson MA, Willson TM, Moore JT, Kliewer SA: The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions. J Clin Invest. 1998 Sep 1;102(5):1016-23. [PubMed Link Image]
  5. Bertilsson G, Heidrich J, Svensson K, Asman M, Jendeberg L, Sydow-Backman M, Ohlsson R, Postlind H, Blomquist P, Berkenstam A: Identification of a human nuclear receptor defines a new signaling pathway for CYP3A induction. Proc Natl Acad Sci U S A. 1998 Oct 13;95(21):12208-13. [PubMed Link Image]
  6. Blumberg B, Sabbagh W Jr, Juguilon H, Bolado J Jr, van Meter CM, Ong ES, Evans RM: SXR, a novel steroid and xenobiotic-sensing nuclear receptor. Genes Dev. 1998 Oct 15;12(20):3195-205. [PubMed Link Image]
Target 7 Drug References
  1. Rabovsky A, Cuomo J, Eich N: Measurement of plasma antioxidant reserve after supplementation with various antioxidants in healthy subjects. Clin Chim Acta. 2006 Sep;371(1-2):55-60. Epub 2006 Mar 6. [PubMed Link Image]
  2. Meijerman I, Beijnen JH, Schellens JH: Herb-drug interactions in oncology: focus on mechanisms of induction. Oncologist. 2006 Jul-Aug;11(7):742-52. [PubMed Link Image]
Drug Target 8 [top]
Target 8 ID 1970
Target 8 Name Protein kinase C alpha type
Target 8 Synonyms
  1. EC 2.7.11.13
  2. PKC-A
  3. PKC-alpha
Target 8 Gene Name PRKCA
Target 8 Protein Sequence >Protein kinase C alpha type 
MADVFPGNDSTASQDVANRFARKGALRQKNVHEVKDHKFIARFFKQPTFCSHCTDFIWGF
GKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPDTDDPRSKHKFKIHTYGSPTFCDHCGS
LLYGLIHQGMKCDTCDMNVHKQCVINVPSLCGMDHTEKRGRIYLKAEVADEKLHVTVRDA
KNLIPMDPNGLSDPYVKLKLIPDPKNESKQKTKTIRSTLNPQWNESFTFKLKPSDKDRRL
SVEIWDWDRTTRNDFMGSLSFGVSELMKMPASGWYKLLNQEEGEYYNVPIPEGDEEGNME
LRQKFEKAKLGPAGNKVISPSEDRKQPSNNLDRVKLTDFNFLMVLGKGSFGKVMLADRKG
TEELYAIKILKKDVVIQDDDVECTMVEKRVLALLDKPPFLTQLHSCFQTVDRLYFVMEYV
NGGDLMYHIQQVGKFKEPQAVFYAAEISIGLFFLHKRGIIYRDLKLDNVMLDSEGHIKIA
DFGMCKEHMMDGVTTRTFCGTPDYIAPEIIAYQPYGKSVDWWAYGVLLYEMLAGQPPFDG
EDEDELFQSIMEHNVSYPKSLSKEAVSICKGLMTKHPAKRLGCGPEGERDVREHAFFRRI
DWEKLENREIQPPFKPKVCGKGAENFDKFFTRGQPVLTPPDQLVIANIDQSDFEGFSYVN
PQFVHPILQSAV
Target 8 Number of Residues 683
Target 8 Molecular Weight 76765
Target 8 Theoretical pI 7.05
Target 8 GO Classification
Function
binding
nucleotide binding
purine nucleotide binding
adenyl nucleotide binding
ATP binding
catalytic activity
transferase activity
transferase activity, transferring phosphorus-containing groups
kinase activity
protein kinase activity
protein serine/threonine kinase activity
Process
physiological process
metabolism
macromolecule metabolism
biopolymer metabolism
biopolymer modification
protein modification
protein amino acid phosphorylation
cellular process
cell communication
signal transduction
intracellular signaling cascade
Component
Not Available
Target 8 General Function Involved in protein serine/threonine kinase activity
Target 8 Specific Function PKC is activated by diacylglycerol which in turn phosphorylates a range of cellular proteins. PKC also serves as the receptor for phorbol esters, a class of tumor promoters
Target 8 Pathways Not Available
Target 8 Reactions
  • ATP + a protein = ADP + a phosphoprotein
Target 8 Pfam Domain Function
Target 8 Signals
  • None
Target 8 Transmembrane Regions
  • None
Target 8 Essentiality Non-Essential
Target 8 GenBank ID Protein 35483 Link Image
Target 8 UniProtKB/Swiss-Prot ID P17252 Link Image
Target 8 UniProtKB/Swiss-Prot Entry Name KPCA_HUMAN Link Image
Target 8 PDB ID Not Available
Target 8 Cellular Location Not Available
Target 8 Gene Sequence >2019 bp 
ATGGCTGACGTTTTCCCGGGCAACGACTCCACGGCGTCTCAGGACGTGGCCAACCGCTTC
GCCCGCAAAGGGGCGCTGAGGCAGAAGAACGTGCACGAGGTGAAGGACCACAAATTCATC
GCGCGCTTCTTCAAGCAGCCCACCTTCTGCAGCCACTGCACCGACTTCATCTGGGGGTTT
GGGAAACAAGGCTTCCAGTGCCAAGTTTGCTGTTTTGTGGTCCACAAGAGGTGCCATGAA
TTTGTTACTTTTTCTTGTCCGGGTGCGGATAAGGGACCCGACACTGATGACCCCAGGAGC
AAGCACAAGTTCAAAATCCACACTTACGGAAGCCCCACCTTCTGCGATCACTGTGGGTCA
CTGCTCTATGGACTTATCCATCAAGGGATGAAATGTGACACCTGCGATATGAACGTTCAC
AAGCAATGCGTCATCAATGTCCCCAGCCTCTGCGGAATGGATCACACTGAGAAGAGGGGG
CGGATTTACCTAAAGGCTGAGGTTGCTGATGAAAAGCTCCATGTCACAGTACGAGATGCA
AAAAATCTAATCCCTATGGATCCAAACGGGCTTTCAGATCCTTATGTGAAGCTGAAACTT
ATTCCTGATCCCAAGAATGAAAGCAAGCAAAAAACCAAAACCATCCGCTCCACACTAAAT
CCGCAGTGGAATGAGTCCTTTACATTCAAATTGAAACCTTCAGACAAAGACCGACGACTG
TCTGTAGAAATCTGGGACTGGGATCGAACAACAAGGAATGACTTCATGGGATCCCTTTCC
TTTGGAGTTTCGGAGCTGATGAAGATGCCGGCCAGTGGATGGTACAAGTTGCTTAACCAA
GAAGAAGGTGAGTACTACAACGTACCCATTCCGGAAGGGGACGAGGAAGGAAACATGGAA
CTCAGGCAGAAATTCGAGAAAGCCAAACTTGGCCCTGCTGGCAACAAAGTCATCAGTCCC
TCTGAAGACAGGAAACAACCTTCCAACAACCTTGACCGAGTGAAACTCACGGACTTCAAT
TTCCTCATGGTGTTGGGAAAGGGGAGTTTTGGAAAGGTGATGCTTGCCGACAGGAAGGGC
ACAGAAGAACTGTATGCAATCAAAATCCTGAAGAAGGATGTGGTGATTCAGGATGATGAC
GTGGAGTGCACCATGGTAGAAAAGCGAGTCTTGGCCCTGCTTGACAAACCCCCGTTCTTG
ACGCAGCTGCACTCCTGCTTCCAGACAGTGGATCGGCTGTACTTCGTCATGGAATATGTC
AACGGTGGGGACCTCATGTACCACATTCAGCAAGTAGGAAAATTTAAGGAACCACAAGCA
GTATTCTATGCGGCAGAGATTTCCATCGGATTGTTCTTTCTTCATAAAAGAGGAATCATT
TATAGGGATCTGAAGTTAGATAACGTCATGTTGGATTCAGAAGGACATATCAAAATTGCT
GACTTTGGGATGTGCAAGGAACACATGATGGATGGAGTCACGACCAGGACCTTCTGTGGG
ACTCCAGATTATATCGCCCCAGAGATAATCGCTTATCAGCCGTATGGAAAATCTGTGGAC
TGGTGGGCCTATGGCGTCCTGTTGTATGAAATGCTTGCCGGGCAGCCTCCATTTGATGGT
GAAGATGAAGACGAGCTATTTCAGTCTATCATGGAGCACAACGTTTCCTATCCAAAATCC
TTGTCCAAGGAGGCTGTTTCTATCTGCAAAGGACTGATGACCAAACACCCAGCCAAGCGG
CTGGGCTGTGGGCCTGAGGGGGAGAGGGACGTGAGAGAGCATGCCTTCTTCCGGAGGATC
GACTGGGAAAAACTGGAGAACAGGGAGATCCAGCCACCATTCAAGCCCAAAGTGTGTGGC
AAAGGAGCAGAGAACTTTGACAAGTTCTTCACACGAGGACAGCCCGTCTTAACACCACCT
GATCAGCTGGTTATTGCTAACATAGACCAGTCTGATTTTGAAGGGTTCTCGTATGTCAAC
CCCCAGTTTGTGCACCCCATCTTACAGAGTGCAGTATGA
Target 8 GenBank Gene ID
Target 8 GeneCard ID PRKCA Link Image
Target 8 GenAtlas ID PRKCA Link Image
Target 8 HGNC ID HGNC:9393 Link Image
Target 8 Chromosome Location 17
Target 8 Locus 17q22-q23.2
Target 8 SNPs SNPJam Report Link Image
Target 8 General References
  1. Gevaert K, Goethals M, Martens L, Van Damme J, Staes A, Thomas GR, Vandekerckhove J: Exploring proteomes and analyzing protein processing by mass spectrometric identification of sorted N-terminal peptides. Nat Biotechnol. 2003 May;21(5):566-9. Epub 2003 Mar 31. [PubMed Link Image]
  2. Zemlickova E, Dubois T, Kerai P, Clokie S, Cronshaw AD, Wakefield RI, Johannes FJ, Aitken A: Centaurin-alpha(1) associates with and is phosphorylated by isoforms of protein kinase C. Biochem Biophys Res Commun. 2003 Aug 1;307(3):459-65. [PubMed Link Image]
  3. McSwine-Kennick RL, McKeegan EM, Johnson MD, Morin MJ: Phorbol diester-induced alterations in the expression of protein kinase C isozymes and their mRNAs. Analysis in wild-type and phorbol diester-resistant HL-60 cell clones. J Biol Chem. 1991 Aug 15;266(23):15135-43. [PubMed Link Image]
  4. Finkenzeller G, Marme D, Hug H: Sequence of human protein kinase C alpha. Nucleic Acids Res. 1990 Apr 25;18(8):2183. [PubMed Link Image]
Target 8 Drug References
  1. Sylvester PW, McIntyre BS, Gapor A, Briski KP: Vitamin E inhibition of normal mammary epithelial cell growth is associated with a reduction in protein kinase C(alpha) activation. Cell Prolif. 2001 Dec;34(6):347-57. [PubMed Link Image]
  2. Huang Y, Ishizuka T, Miura A, Kajita K, Ishizawa M, Kimura M, Yamamoto Y, Kawai Y, Morita H, Uno Y, Yasuda K: Effect of 1 alpha,25-dihydroxy vitamin D3 and vitamin E on insulin-induced glucose uptake in rat adipocytes. Diabetes Res Clin Pract. 2002 Mar;55(3):175-83. [PubMed Link Image]
  3. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  4. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
  5. Azzi A, Boscoboinik D, Clement S, Marilley D, Ozer NK, Ricciarelli R, Tasinato A: Alpha-tocopherol as a modulator of smooth muscle cell proliferation. Prostaglandins Leukot Essent Fatty Acids. 1997 Oct;57(4-5):507-14. [PubMed Link Image]
Drug Target 9 [top]
Target 9 ID 4076
Target 9 Name Diacylglycerol kinase alpha
Target 9 Synonyms
  1. 80 kDa diacylglycerol kinase
  2. DAG kinase alpha
  3. DGK-alpha
  4. Diglyceride kinase alpha
  5. EC 2.7.1.107
Target 9 Gene Name DGKA
Target 9 Protein Sequence >Diacylglycerol kinase alpha 
MAKERGLISPSDFAQLQKYMEYSTKKVSDVLKLFEDGEMAKYVQGDAIGYEGFQQFLKIY
LEVDNVPRHLSLALFQSFETGHCLNETNVTKDVVCLNDVSCYFSLLEGGRPEDKLEFTFK
LYDTDRNGILDSSEVDKIILQMMRVAEYLDWDVSELRPILQEMMKEIDYDGSGSVSQAEW
VRAGATTVPLLVLLGLEMTLKDDGQHMWRPKRFPRPVYCNLCESSIGLGKQGLSCNLCKY
TVHDQCAMKALPCEVSTYAKSRKDIGVQSHVWVRGGCESGRCDRCQKKIRIYHSLTGLHC
VWCHLEIHDDCLQAVGHECDCGLLRDHILPPSSIYPSVLASGPDRKNSKTSQKTMDDLNL
STSEALRIDPVPNTHPLLVFVNPKSGGKQGQRVLWKFQYILNPRQVFNLLKDGPEIGLRL
FKDVPDSRILVCGGDGTVGWILETIDKANLPVLPPVAVLPLGTGNDLARCLRWGGGYEGQ
NLAKILKDLEMSKVVHMDRWSVEVIPQQTEEKSDPVPFQIINNYFSIGVDASIAHRFHIM
REKYPEKFNSRMKNKLWYFEFATSESIFSTCKKLEESLTVEICGKPLDLSNLSLEGIAVL
NIPSMHGGSNLWGDTRRPHGDIYGINQALGATAKVITDPDILKTCVPDLSDKRLEVVGLE
GAIEMGQIYTKLKNAGRRLAKCSEITFHTTKTLPMQIDVEPWMQTPCTIKITHKNQMPML
MGPPPRSTNFFGFLS
Target 9 Number of Residues 747
Target 9 Molecular Weight 82673
Target 9 Theoretical pI 6.71
Target 9 GO Classification
Function
binding
ion binding
cation binding
calcium ion binding
catalytic activity
transferase activity
transferase activity, transferring phosphorus-containing groups
kinase activity
diacylglycerol kinase activity
Process
G-protein signaling, coupled to IP3 second messenger (phospholipase C activating)
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
G-protein signaling, coupled to IP3 second messenger (phospholipase C activating)
protein kinase C activation
cellular process
cell communication
signal transduction
intracellular signaling cascade
Component
Not Available
Target 9 General Function Not Available
Target 9 Specific Function Upon cell stimulation converts the second messenger diacylglycerol into phosphatidate, initiating the resynthesis of phosphatidylinositols and attenuating protein kinase C activity
Target 9 Pathways
Name SMPDB Link KEGG Link
Phosphatidylinositol signaling system map00561 Link Image
Target 9 Reactions
  • ATP + 1,2-diacylglycerol = ADP + 1,2-diacyl-sn-glycerol 3-phosphate
Target 9 Pfam Domain Function
Target 9 Signals
  • None
Target 9 Transmembrane Regions
  • None
Target 9 Essentiality Non Essential
Target 9 GenBank ID Protein 30823 Link Image
Target 9 UniProtKB/Swiss-Prot ID P23743 Link Image
Target 9 UniProtKB/Swiss-Prot Entry Name DGKA_HUMAN Link Image
Target 9 PDB ID 1TUZ Link Image
Target 9 PDB File Show
Target 9 3D Structure
Target 9 Cellular Location Not Available
Target 9 Gene Sequence >2208 bp 
ATGGCCAAGGAGAGGGGCCTAATAAGCCCCAGTGATTTTGCCCAGCTGCAAAAATACATG
GAATACTCCACCAAAAAGGTCAGTGATGTCCTAAAGCTCTTCGAGGATGGCGAGATGGCT
AAATATGTCCAAGGAGATGCCATTGGGTACGAGGGATTCCAGCAATTCCTGAAAATCTAT
CTCGAAGTGGATAATGTTCCCAGACACCTAAGCCTGGCACTGTTTCAATCCTTTGAGACT
GGTCACTGCTTAAATGAGACAAATGTGACAAAAGATGTGGTGTGTCTCAATGATGTTTCC
TGCTACTTTTCCCTTCTGGAGGGTGGTCGGCCAGAAGACAAGTTAGAATTCACCTTCAAG
CTGTACGACACGGACAGAAATGGGATCCTGGACAGCTCAGAAGTGGACAAAATTATCCTA
CAGATGATGCGAGTGGCTGAATACCTGGATTGGGATGTGTCTGAGCTGAGGCCGATTCTT
CAGGAGATGATGAAAGAGATTGACTATGATGGCAGTGGCTCTGTCTCTCAAGCTGAGTGG
GTCCGGGCTGGGGCCACCACCGTGCCACTGCTAGTGCTGCTGGGTCTGGAGATGACTCTG
AAGGACGACGGACAGCACATGTGGAGGCCCAAGAGGTTCCCCAGACCAGTCTACTGCAAT
CTGTGCGAGTCAAGCATTGGTCTTGGCAAACAGGGACTGAGCTGTAACCTCTGTAAGTAC
ACTGTTCACGACCAGTGTGCCATGAAAGCCCTGCCTTGTGAAGTCAGCACCTATGCCAAG
TCTCGGAAGGACATTGGTGTCCAATCACATGTGTGGGTGCGAGGAGGCTGTGAGTCCGGG
CGCTGCGACCGCTGTCAGAAAAAGATCCGGATCTACCACAGTCTGACCGGGCTGCATTGT
GTATGGTGCCACCTAGAGATCCACGATGACTGCCTGCAAGCGGTGGGCCATGAGTGTGAC
TGTGGGCTGCTCCGGGATCACATCCTGCCTCCATCTTCCATCTATCCCAGTGTCCTGGCC
TCTGGACCGGATCGTAAAAATAGCAAAACAAGCCAGAAGACCATGGATGATTTAAATTTG
AGCACCTCTGAGGCTCTGCGGATTGACCCTGTTCCTAACACCCACCCACTTCTCGTCTTT
GTCAATCCTAAGAGTGGCGGGAAGCAGGGGCAGAGGGTGCTCTGGAAGTTCCAGTATATA
TTAAACCCTCGACAGGTGTTCAACCTCCTAAAGGATGGTCCTGAGATAGGGCTCCGATTA
TTCAAGGATGTTCCTGATAGCCGGATTTTGGTGTGTGGTGGAGACGGCACAGTAGGCTGG
ATTCTAGAGACCATTGACAAAGCTAACTTGCCAGTTTTGCCTCCTGTTGCTGTGTTGCCC
CTGGGTACTGGAAATGATCTGGCTCGATGCCTAAGATGGGGAGGAGGTTATGAAGGACAG
AATCTGGCAAAGATCCTCAAGGATTTAGAGATGAGTAAAGTGGTACATATGGATCGATGG
TCTGTGGAGGTGATACCTCAACAAACTGAAGAAAAAAGTGACCCAGTCCCCTTTCAAATC
ATCAATAACTACTTCTCTATTGGCGTGGATGCCTCTATTGCTCATCGATTCCACATCATG
CGAGAGAAATATCCGGAGAAGTTCAACAGCAGAATGAAGAACAAGCTATGGTACTTCGAA
TTTGCCACATCTGAATCCATCTTCTCAACATGCAAAAAGCTGGAGGAGTCTTTGACAGTT
GAGATCTGTGGGAAACCGCTGGATCTGAGCAACCTGTCCCTAGAAGGCATCGCAGTGCTA
AACATCCCTAGCATGCATGGTGGCTCCAACCTCTGGGGTGATACCAGGAGACCCCATGGG
GATATCTATGGGATCAACCAGGCCTTAGGTGCTACAGCTAAAGTCATCACCGACCCTGAT
ATCCTGAAAACCTGTGTACCAGACCTAAGTGACAAGAGACTGGAAGTGGTTGGGCTGGAG
GGTGCAATTGAGATGGGCCAAATCTATACCAAGCTCAAGAATGCTGGACGTCGGCTGGCC
AAGTGCTCTGAGATCACCTTCCACACCACAAAAACCCTTCCCATGCAAATTGACGTAGAA
CCCTGGATGCAGACGCCCTGTACAATCAAGATCACCCACAAGAACCAGATGCCCATGCTC
ATGGGCCCACCCCCCCGCTCCACCAATTTCTTTGGCTTCTTGAGCTAA
Target 9 GenBank Gene ID
Target 9 GeneCard ID DGKA Link Image
Target 9 GenAtlas ID DGKA Link Image
Target 9 HGNC ID HGNC:2849 Link Image
Target 9 Chromosome Location 12
Target 9 Locus 12q13.3
Target 9 SNPs SNPJam Report Link Image
Target 9 General References
  1. Schaap D, de Widt J, van der Wal J, Vandekerckhove J, van Damme J, Gussow D, Ploegh HL, van Blitterswijk WJ, van der Bend RL: Purification, cDNA-cloning and expression of human diacylglycerol kinase. FEBS Lett. 1990 Nov 26;275(1-2):151-8. [PubMed Link Image]
  2. Hart TC, Zhou J, Champagne C, Van Dyke TE, Rao PN, Pettenati MJ: Assignment of the human diacylglycerol kinase gene (DAGK) to 12q13.3 using fluorescence in situ hybridization analysis. Genomics. 1994 Jul 1;22(1):246-7. [PubMed Link Image]
  3. Hart TC, Champagne C, Zhou J, Van Dyke TE: Assignment of the gene for diacylglycerol kinase (DAGK) to human chromosome 12. Mamm Genome. 1994 Feb;5(2):123-4. [PubMed Link Image]
Target 9 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 10 [top]
Target 10 ID 4077
Target 10 Name Serine/threonine-protein phosphatase 2A catalytic subunit beta isoform
Target 10 Synonyms
  1. EC 3.1.3.16
  2. PP2A-beta
Target 10 Gene Name PPP2CB
Target 10 Protein Sequence >Serine/threonine-protein phosphatase 2A catalytic subunit beta isoform 
MDDKAFTKELDQWVEQLNECKQLNENQVRTLCEKAKEILTKESNVQEVRCPVTVCGDVHG
QFHDLMELFRIGGKSPDTNYLFMGDYVDRGYYSVETVTLLVALKVRYPERITILRGNHES
RQITQVYGFYDECLRKYGNANVWKYFTDLFDYLPLTALVDGQIFCLHGGLSPSIDTLDHI
RALDRLQEVPHEGPMCDLLWSDPDDRGGWGISPRGAGYTFGQDISETFNHANGLTLVSRA
HQLVMEGYNWCHDRNVVTIFSAPNYCYRCGNQAAIMELDDTLKYSFLQFDPAPRRGEPHV
TRRTPDYFL
Target 10 Number of Residues 314
Target 10 Molecular Weight 35575
Target 10 Theoretical pI 5.08
Target 10 GO Classification
Function
catalytic activity
hydrolase activity
Process
Not Available
Component
Not Available
Target 10 General Function Signal transduction mechanisms
Target 10 Specific Function PP2A can modulate the activity of phosphorylase B kinase casein kinase 2, mitogen-stimulated S6 kinase, and MAP-2 kinase
Target 10 Pathways
Name SMPDB Link KEGG Link
Insulin signaling pathway map04010 Link Image
Target 10 Reactions
  • a phosphoprotein + H2O = a protein + phosphate
Target 10 Pfam Domain Function
Target 10 Signals
  • None
Target 10 Transmembrane Regions
  • None
Target 10 Essentiality Non Essential
Target 10 GenBank ID Protein 35581 Link Image
Target 10 UniProtKB/Swiss-Prot ID P62714 Link Image
Target 10 UniProtKB/Swiss-Prot Entry Name PP2AB_HUMAN Link Image
Target 10 PDB ID Not Available
Target 10 Cellular Location
  • Cytoplasm
Target 10 Gene Sequence >930 bp 
ATGGACGACAAGGCGTTCACCAAGGAGCTGGACCAGTGGGTCGAGCAGCTGAACGAGTGT
AAGCAGCTGAACGAGAACCAAGTGCGGACGCTGTGCGAGAAGGCAAAGGAAATTTTAACA
AAAGAATCAAATGTGCAAGAGGTTCGTTGCCCTGTTACTGTCTGTGGAGATGTGCATGGT
CAATTTCATGATCTTATGGAACTCTTTAGAATTGGTGGAAAATCACCGGATACAAACTAC
TTATTCATGGGTGACTATGTAGACAGAGGATATTATTCAGTGGAGACTGTGACTCTTCTT
GTAGCATTAAAGGTGCGTTATCCAGAACGCATTACAATATTGAGAGGAAATCACGAAAGC
CGACAAATTACCCAAGTATATGGCTTTTATGATGAATGTCTGCGAAAGTATGGGAATGCC
AACGTTTGGAAATATTTTACAGATCTCTTTGATTATCTTCCACTTACAGCTTTAGTAGAT
GGACAGATATTCTGCCTCCATGGTGGCCTCTCTCCATCCATAGACACACTGGATCATATA
AGAGCCCTGGATCGTTTACAGGAAGTTCCACATGAGGGCCCAATGTGTGATCTGTTATGG
TCAGATCCAGATGATCGTGGTGGATGGGGTATTTCACCACGTGGTGCTGGCTACACATTT
GGACAAGACATTTCTGAAACCTTTAACCATGCCAATGGTCTCACACTGGTTTCTCGTGCC
CACCAGCTTGTAATGGAGGGATACAATTGGTGTCATGATCGGAATGTGGTTACCATTTTC
AGTGCACCCAATTACTGTTATCGTTGTGGGAACCAGGCTGCTATCATGGAATTAGATGAC
ACTTTAAAATATTCCTTCCTTCAATTTGACCCGGCGCCTCGTCGTGGTGAGCCTCATGTT
ACACGGCGCACCCCAGACTACTTCCTATAA
Target 10 GenBank Gene ID
Target 10 GeneCard ID PPP2CB Link Image
Target 10 GenAtlas ID PPP2CB Link Image
Target 10 HGNC ID HGNC:9300 Link Image
Target 10 Chromosome Location 8
Target 10 Locus 8p12
Target 10 SNPs SNPJam Report Link Image
Target 10 General References
  1. Ogris E, Du X, Nelson KC, Mak EK, Yu XX, Lane WS, Pallas DC: A protein phosphatase methylesterase (PME-1) is one of several novel proteins stably associating with two inactive mutants of protein phosphatase 2A. J Biol Chem. 1999 May 14;274(20):14382-91. [PubMed Link Image]
  2. Khew-Goodall Y, Mayer RE, Maurer F, Stone SR, Hemmings BA: Structure and transcriptional regulation of protein phosphatase 2A catalytic subunit genes. Biochemistry. 1991 Jan 8;30(1):89-97. [PubMed Link Image]
  3. Pallas DC, Shahrik LK, Martin BL, Jaspers S, Miller TB, Brautigan DL, Roberts TM: Polyoma small and middle T antigens and SV40 small t antigen form stable complexes with protein phosphatase 2A. Cell. 1990 Jan 12;60(1):167-76. [PubMed Link Image]
  4. Virshup DM, Kauffman MG, Kelly TJ: Activation of SV40 DNA replication in vitro by cellular protein phosphatase 2A. EMBO J. 1989 Dec 1;8(12):3891-8. [PubMed Link Image]
  5. Arino J, Woon CW, Brautigan DL, Miller TB Jr, Johnson GL: Human liver phosphatase 2A: cDNA and amino acid sequence of two catalytic subunit isotypes. Proc Natl Acad Sci U S A. 1988 Jun;85(12):4252-6. [PubMed Link Image]
  6. Hemmings BA, Wernet W, Mayer R, Maurer F, Hofsteenge J, Stone SR: The nucleotide sequence of the cDNA encoding the human lung protein phosphatase 2A beta catalytic subunit. Nucleic Acids Res. 1988 Dec 9;16(23):11366. [PubMed Link Image]
  7. Favre B, Zolnierowicz S, Turowski P, Hemmings BA: The catalytic subunit of protein phosphatase 2A is carboxyl-methylated in vivo. J Biol Chem. 1994 Jun 10;269(23):16311-7. [PubMed Link Image]
Target 10 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 11 [top]
Target 11 ID 4078
Target 11 Name Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoform
Target 11 Synonyms
  1. EC 3.1.3.16
  2. PP2A-alpha
  3. RP-C
  4. Replication protein C
Target 11 Gene Name PPP2CA
Target 11 Protein Sequence >Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoform 
MDEKVFTKELDQWIEQLNECKQLSESQVKSLCEKAKEILTKESNVQEVRCPVTVCGDVHG
QFHDLMELFRIGGKSPDTNYLFMGDYVDRGYYSVETVTLLVALKVRYRERITILRGNHES
RQITQVYGFYDECLRKYGNANVWKYFTDLFDYLPLTALVDGQIFCLHGGLSPSIDTLDHI
RALDRLQEVPHEGPMCDLLWSDPDDRGGWGISPRGAGYTFGQDISETFNHANGLTLVSRA
HQLVMEGYNWCHDRNVVTIFSAPNYCYRCGNQAAIMELDDTLKYSFLQFDPAPRRGEPHV
TRRTPDYFL
Target 11 Number of Residues 314
Target 11 Molecular Weight 35595
Target 11 Theoretical pI 5.22
Target 11 GO Classification
Function
catalytic activity
hydrolase activity
Process
Not Available
Component
Not Available
Target 11 General Function Signal transduction mechanisms
Target 11 Specific Function PP2A can modulate the activity of phosphorylase B kinase casein kinase 2, mitogen-stimulated S6 kinase, and MAP-2 kinase. Can dephosphorylate SV40 large T antigen and p53. Dephosphorylates SV40 large T antigen, preferentially on serine residues 120, 123, 677, and perhaps 679. The C subunit was most active, followed by the AC form, which was more active than the ABC form, and activity of all three forms was strongly stimulated by manganese, and to a lesser extent by magnesium. Dephosphorylation by the AC form, but not C or ABC form is inhibited by small T antigen
Target 11 Pathways
Name SMPDB Link KEGG Link
Insulin signaling pathway map04010 Link Image
Target 11 Reactions
  • a phosphoprotein + H2O = a protein + phosphate
Target 11 Pfam Domain Function
Target 11 Signals
  • None
Target 11 Transmembrane Regions
  • None
Target 11 Essentiality Non Essential
Target 11 GenBank ID Protein 36120 Link Image
Target 11 UniProtKB/Swiss-Prot ID P67775 Link Image
Target 11 UniProtKB/Swiss-Prot Entry Name PP2AA_HUMAN Link Image
Target 11 PDB ID Not Available
Target 11 Cellular Location
  • Cytoplasm
Target 11 Gene Sequence >930 bp 
ATGGACGAGAAGGTGTTCACCAAGGAGCTGGACCAGTGGATCGAGCAGCTGAACGAGTGC
AAGCAGCTGTCCGAGTCCCAGGTCAAGAGCCTCTGCGAGAAGGCTAAAGAAATCCTGACA
AAAGAATCCAACGTGCAAGAGGTTCGATGTCCAGTTACTGTCTGTGGAGATGTGCATGGG
CAATTTCATGATCTCATGGAACTGTTTAGAATTGGTGGCAAATCACCAGATACAAATTAC
TTGTTTATGGGAGATTATGTTGACAGAGGATATTATTCAGTTGAAACAGTTACACTGCTT
GTAGCTCTTAAGGTTCGTTACCGTGAACGCATCACCATTCTTCGAGGGAATCATGAGAGC
AGACAGATCACACAAGTTTATGGTTTCTATGATGAATGTTTAAGAAAATATGGAAATGCA
AATGTTTGGAAATATTTTACAGATCTTTTTGACTATCTTCCTCTCACTGCCTTGGTGGAT
GGGCAGATCTTCTGTCTACATGGTGGTCTCTCGCCATCTATAGATACACTGGATCATATC
AGAGCACTTGATCGCCTACAAGAAGTTCCCCATGAGGGTCCAATGTGTGACTTGCTGTGG
TCAGATCCAGATGACCGTGGTGGTTGGGGTATATCTCCTCGAGGAGCTGGTTACACCTTT
GGGCAAGATATTTCTGAGACATTTAATCATGCCAATGGCCTCACGTTGGTGTCTAGAGCT
CACCAGCTAGTGATGGAGGGATATAACTGGTGCCATGACCGGAATGTAGTAACGATTTTC
AGTGCTCCAAACTATTGTTATCGTTGTGGTAACCAAGCTGCAATCATGGAACTTGACGAT
ACTCTAAAATACTCTTTCTTGCAGTTTGACCCAGCACCTCGTAGAGGCGAGCCACATGTT
ACTCGTCGTACCCCAGACTACTTCCTGTAA
Target 11 GenBank Gene ID
Target 11 GeneCard ID PPP2CA Link Image
Target 11 GenAtlas ID PPP2CA Link Image
Target 11 HGNC ID HGNC:9299 Link Image
Target 11 Chromosome Location 5
Target 11 Locus 5q31.1
Target 11 SNPs SNPJam Report Link Image
Target 11 General References
  1. Bryant JC, Westphal RS, Wadzinski BE: Methylated C-terminal leucine residue of PP2A catalytic subunit is important for binding of regulatory Balpha subunit. Biochem J. 1999 Apr 15;339 ( Pt 2):241-6. [PubMed Link Image]
  2. Khew-Goodall Y, Mayer RE, Maurer F, Stone SR, Hemmings BA: Structure and transcriptional regulation of protein phosphatase 2A catalytic subunit genes. Biochemistry. 1991 Jan 8;30(1):89-97. [PubMed Link Image]
  3. Scheidtmann KH, Virshup DM, Kelly TJ: Protein phosphatase 2A dephosphorylates simian virus 40 large T antigen specifically at residues involved in regulation of DNA-binding activity. J Virol. 1991 Apr;65(4):2098-101. [PubMed Link Image]
  4. Scheidtmann KH, Mumby MC, Rundell K, Walter G: Dephosphorylation of simian virus 40 large-T antigen and p53 protein by protein phosphatase 2A: inhibition by small-t antigen. Mol Cell Biol. 1991 Apr;11(4):1996-2003. [PubMed Link Image]
  5. Virshup DM, Kauffman MG, Kelly TJ: Activation of SV40 DNA replication in vitro by cellular protein phosphatase 2A. EMBO J. 1989 Dec 1;8(12):3891-8. [PubMed Link Image]
  6. Arino J, Woon CW, Brautigan DL, Miller TB Jr, Johnson GL: Human liver phosphatase 2A: cDNA and amino acid sequence of two catalytic subunit isotypes. Proc Natl Acad Sci U S A. 1988 Jun;85(12):4252-6. [PubMed Link Image]
  7. Stone SR, Mayer R, Wernet W, Maurer F, Hofsteenge J, Hemmings BA: The nucleotide sequence of the cDNA encoding the human lung protein phosphatase 2A alpha catalytic subunit. Nucleic Acids Res. 1988 Dec 9;16(23):11365. [PubMed Link Image]
  8. Favre B, Zolnierowicz S, Turowski P, Hemmings BA: The catalytic subunit of protein phosphatase 2A is carboxyl-methylated in vivo. J Biol Chem. 1994 Jun 10;269(23):16311-7. [PubMed Link Image]
Target 11 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.