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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-06-23 18:06:34
Primary Accession Number DB01028
Secondary Accession Number
  • APRD00744
Name Methoxyflurane
Drug Type
  • Approved
  • Small Molecule
Description An inhalation anesthetic. Currently, methoxyflurane is rarely used for surgical, obstetric, or dental anesthesia. If so employed, it should be administered with nitrous oxide to achieve a relatively light level of anesthesia, and a neuromuscular blocking agent given concurrently to obtain the desired degree of muscular relaxation. (From AMA Drug Evaluations Annual, 1994, p180)
Synonyms
  1. MOF
  2. Methoflurane
  3. Methoxiflurane
  4. Methoxifluranum
  5. Methoxyfluoran
  6. Methoxyfluorane
  7. Methoxyfluran
  8. Methoxyfluranum [INN-Latin]
  9. Metossiflurano [Dcit]
  10. Metoxfluran
  11. Metoxifluran
  12. Metoxiflurano [INN-Spanish]
Brand Names
  1. Analgizer
  2. Anecotan
  3. Ingalan
  4. Inhalan
  5. Methofane
  6. Methoxane
  7. Metofane
  8. Penthrane
  9. Pentran
  10. Pentrane
Brand Mixtures Not Available
Chemical IUPAC Name 2,2-dichloro-1,1-difluoro-1-methoxyethane
Chemical Formula C3H4Cl2F2O
Chemical Structure Structure
CAS Registry Number 76-38-0
InChI Identifier InChI=1/C3H4Cl2F2O/c1-8-3(6,7)2(4)5/h2H,1H3
InChI Key RFKMCNOHBTXSMU-UHFFFAOYAI
KEGG Drug D00544 Link Image
KEGG Compound C07517 Link Image
PubChem Compound 4116 Link Image
PubChem Substance 149389 Link Image
ChEBI ID Not Available
PharmGKB ID PA450434 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 02019027 Link Image
RxList Link Not Available
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Methoxyflurane Link Image
FDA Label Not Available
Material Safety Data Sheet (MSDS)
Synthesis Reference Miller et al., J. Am. Chem. Soc. 70, 431 (1948)
Average Molecular Weight 164.9660
Monoisotopic Molecular Weight 163.9607
State Liquid
Melting Point -35 oC (melting point), 105 oC (boiling point)
Experimental Water Solubility 2.83E+004 mg/L Source: PhysProp
Predicted Water Solubility 6.46e+00 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 1.8 Source: PhysProp
Predicted LogP 2.01 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -1.41 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 Not Available
Isomeric SMILES COC(F)(F)C(Cl)Cl
Canonical SMILES COC(F)(F)C(Cl)Cl
Drug Category
  • Anesthetics, Inhalation
ATC Codes
AHFS Codes Not Available
Indication For use in the induction and maintenance of general anesthesia
Pharmacology Methoxyflurane is a general inhalation anesthetic used for induction and maintenance of general anesthesia. It induces muscle relaxation and reduces pains sensitivity by altering tissue excitability. It does so by decreasing the extent of gap junction mediated cell-cell coupling and altering the activity of the channels that underlie the action potential.
Mechanism of Action Methoxyflurane induces a reduction in junctional conductance by decreasing gap junction channel opening times and increasing gap junction channel closing times. Methoxyflurane also activates calcium dependent ATPase in the sarcoplasmic reticulum by increasing the fluidity of the lipid membrane. It also appears to bind the D subunit of ATP synthase and NADH dehydogenase. Methoxyflurane also binds to the GABA receptor, the large conductance Ca2+ activated potassium channel, the glutamate receptor and the glycine receptor.
Absorption Not Available
Toxicity LD50=3600 mg/kg (Orally in rats). Symptoms of overexposure include eye irritation, CNS depression, analgesia, anesthesia, seizures, respiratory depression, and liver and kidney damage.
Protein Binding Not Available
Biotransformation Hepatic.
Half Life Not Available
Dosage Forms Not Available
Patient Information Not Available
Contraindications Not Available
Interactions Not Available
Drug Interactions Not Available
Food Interactions Not Available
Pathways Not Available
General References
  1. Drugs.com Link Image
  2. Wikipedia Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. Cytochrome P450 2E1 (CYP2E1)
  2. NADPH-cytochrome P450 reductase
Targets
  1. Calcium-transporting ATPase type 2C member 1
  2. Glycine receptor subunit alpha-1
  3. ATP synthase delta chain, mitochondrial
  4. NADH-ubiquinone oxidoreductase chain 1
  5. Glutamate receptor 1
  6. Potassium voltage-gated channel subfamily A member 1
  7. Gamma-aminobutyric-acid receptor subunit alpha-1
  8. Cytochrome b5
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 2E1 (CYP2E1)
Enzyme 1 Gene Name CYP2E1
Enzyme 1 SwissProt ID P05181 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P05181|CP2E1_HUMAN Cytochrome P450 2E1 (EC 1.14.14.1) 
MSALGVTVALLVWAAFLLLVSMWRQVHSSWNLPPGPFPLPIIGNLFQLELKNIPKSFTRL
AQRFGPVFTLYVGSQRMVVMHGYKAVKEALLDYKDEFSGRGDLPAFHAHRDRGIIFNNGP
TWKDIRRFSLTTLRNYGMGKQGNESRIQREAHFLLEALRKTQGQPFDPTFLIGCAPCNVI
ADILFRKHFDYNDEKFLRLMYLFNENFHLLSTPWLQLYNNFPSFLHYLPGSHRKVIKNVA
EVKEYVSERVKEHHQSLDPNCPRDLTDCLLVEMEKEKHSAERLYTMDGITVTVADLFFAG
TETTSTTLRYGLLILMKYPEIEEKLHEEIDRVIGPSRIPAIKDRQEMPYMDAVVHEIQRF
ITLVPSNLPHEATRDTIFRGYLIPKGTVVVPTLDSVLYDNQEFPDPEKFKPEHFLNENGK
FKYSDYFKPFSTGKRVCAGEGLARMELFLLLCAILQHFNLKPLVDPKDIDLSPIHIGFGC
IPPRYKLCVIPRS
Phase 1 Metabolizing Enzyme 2 [top]
Enzyme 2 Name NADPH-cytochrome P450 reductase
Enzyme 2 Gene Name POR
Enzyme 2 SwissProt ID P16435 Link Image
Enzyme 2 SNPs SNPJam Report Link Image
Enzyme 2 Protein Sequence >sp|P16435|NCPR_HUMAN NADPH--cytochrome P450 reductase 
GDSHVDTSSTVSEAVAEEVSLFSMTDMILFSLIVGLLTYWFLFRKKKEEVPEFTKIQTLT
SSVRESSFVEKMKKTGRNIIVFYGSQTGTAEEFANRLSKDAHRYGMRGMSADPEEYDLAD
LSSLPEIDNALVVFCMATYGEGDPTDNAQDFYDWLQETDVDLSGVKFAVFGLGNKTYEHF
NAMGKYVDKRLEQLGAQRIFELGLGDDDGNLEEDFITWREQFWPAVCEHFGVEATGEESS
IRQYELVVHTDIDAAKVYMGEMGRLKSYENQKPPFDAKNPFLAAVTTNRKLNQGTERHLM
HLELDISDSKIRYESGDHVAVYPANDSALVNQLGKILGADLDVVMSLNNLDEESNKKHPF
PCPTSYRTALTYYLDITNPPRTNVLYELAQYASEPSEQELLRKMASSSGEGKELYLSWVV
EARRHILAILQDCPSLRPPIDHLCELLPRLQARYYSIASSSKVHPNSVHICAVVVEYETK
AGRINKGVATNWLRAKEPAGENGGRALVPMFVRKSQFRLPFKATTPVIMVGPGTGVAPFI
GFIQERAWLRQQGKEVGETLLYYGCRRSDEDYLYREELAQFHRDGALTQLNVAFSREQSH
KVYVQHLLKQDREHLWKLIEGGAHIYVCGDARNMARDVQNTFYDIVAELGAMEHAQAVDY
IKKLMTKGRYSLDVWS
Drug Target 1 [top]
Target 1 ID 241
Target 1 Name Calcium-transporting ATPase type 2C member 1
Target 1 Synonyms
  1. ATP-dependent Ca(2+
  2. ATPase 2C1
  3. EC 3.6.3.8
Target 1 Gene Name ATP2C1
Target 1 Protein Sequence >Calcium-transporting ATPase type 2C member 1 
MKVARFQKIPNGENETMIPVLTSKKASELPVSEVASILQADLQNGLNKCEVSHRRAFHGW
NEFDISEDEPLWKKYISQFKNPLIMLLLASAVISVLMHQFDDAVSITVAILIVVTVAFVQ
EYRSEKSLEELSKLVPPECHCVREGKLEHTLARDLVPGDTVCLSVGDRVPADLRLFEAVD
LSIDESSLTGETTPCSKVTAPQPAATNGDLASRSNIAFMGTLVRCGKAKGVVIGTGENSE
FGEVFKMMQAEEAPKTPLQKSMDLLGKQLSFYSFGIIGIIMLVGWLLGKDILEMFTISVS
LAVAAIPEGLPIVVTVTLALGVMRMVKKRAIVKKLPIVETLGCCNVICSDKTGTLTKNEM
TVTHIFTSDGLHAEVTGVGYNQFGEVIVDGDVVHGFYNPAVSRIVEAGCVCNDAVIRNNT
LMGKPTEGALIALAMKMGLDGLQQDYIRKAEYPFSSEQKWMAVKCVHRTQQDRPEICFMK
GAYEQVIKYCTTYQSKGQTLTLTQQQRDVYQQEKARMGSAGLRVLALASGPELGQLTFLG
LVGIIDPPRTGVKEAVTTLIASGVSIKMITGDSQETAVAIASRLGLYSKTSQSVSGEEID
AMDVQQLSQIVPKVAVFYRASPRHKMKIIKSLQKNGSVVAMTGDGVNDAVALKAADIGVA
MGQTGTDVCKEAADMILVDDDFQTIMSAIEEGKGIYNNIKNFVRFQLSTSIAALTLISLA
TLMNFPNPLNAMQILWINIIMDGPPAQSLGVEPVDKDVIRKPPRNWKDSILTKNLILKIL
VSSIIIVCGTLFVFWRELRDNVITPRDTTMTFTCFVFFDMFNALSSRSQTKSVFEIGLCS
NRMFCYAVLGSIMGQLLVIYFPPLQKVFQTESLSILDLLFLLGLTSSVCIVAEIIKKVER
SREKIQKHVSSTSSSFLEV
Target 1 Number of Residues 934
Target 1 Molecular Weight 100579
Target 1 Theoretical pI 6.72
Target 1 GO Classification
Function
hydrolase activity
hydrolase activity, acting on acid anhydrides
hydrolase activity, acting on acid anhydrides, catalyzing transmembrane movement of substances
catalytic activity
ATPase activity, coupled to transmembrane movement of ions, phosphorylative mechanism
binding
nucleotide binding
purine nucleotide binding
adenyl nucleotide binding
ATP binding
transporter activity
ion transporter activity
cation transporter activity
di-, tri-valent inorganic cation transporter activity
calcium ion transporter activity
calcium-transporting ATPase activity
Process
metabolism
physiological process
cellular physiological process
transport
ion transport
cation transport
di-, tri-valent inorganic cation transport
calcium ion transport
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 1 General Function Inorganic ion transport and metabolism
Target 1 Specific Function This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of the calcium
Target 1 Pathways Not Available
Target 1 Reactions
  • ATP + H2O + Ca2+cis = ADP + phosphate + Ca2+trans
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 71-91
  • 105-123
  • 263-282
  • 295-312
  • 700-719
  • 730-750
  • 771-793
  • 809-828
  • 842-860
  • 876-896
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 6715131 Link Image
Target 1 UniProtKB/Swiss-Prot ID P98194 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name AT2C1_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Golgi apparatus
  • Golgi apparatus membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >2760 bp 
ATGAAGGTTGCACGTTTTCAAAAAATACCTAATGGTGAAAATGAGACAATGATTCCTGTA
TTGACATCAAAAAAAGCAAGTGAATTACCAGTCAGTGAAGTTGCAAGCATTCTCCAAGCT
GATCTTCAGAATGGTCTAAACAAATGTGAAGTTAGTCATAGGCGAGCCTTTCATGGCTGG
AATAAGTTTGATATTAGTGAAGATGAGCCACTGTGGAAGAAGTATATTTCTCAGTTTAAA
AATCCCCTTATTATGCTGCTTCTGGCTTCTGCAGTCATCAGTGTTTTAATGCATCAGTTT
GATGATGCCGTCAGTATCACTGTGGCAATACTTATCGTTGTTACAGTTGCCTTTGTTCAG
GAATATCGTTCAGAAAAATCTCTTGAAGAATTGAGTAAACTTGTGCCACCAGAATGCCAT
TGTGTGCGTGAAGGAAAATTGGAGCATACACTTGCCCGAGACTTGGTTCCAGGTGATACA
GTTTGCCTTTCTGTTGGGGATAGAGTTCCTGCTGACTTACGCTTGTTTGAGGCTGTGGAT
CTTTCCATTGATGAGTCCAGCTTGACAGGTGAGACAACGCCTTGTTCTAAGGTGACAGCT
CCTCAGCCAGCTGCAACTAATGGAGATCTTGCATCGAGAAGTAACATTGCCTTTATGGGA
ACACTGGTCAGATGTGGCAAAGCAAAGGGTGTTGTCATTGGAACAGGAGAAAATTCTGAA
TTTGGGGAGGTTTTTAAAATGATGCAAGCAGAAGAGGCACCAAAAACCCCTCTGCAGAAG
AGCATGGACCTCTTAGGAAAACAACTTTCCTTTTACTCCTTTGGTATAATAGGAATCATC
ATGTTGGTTGGCTGGTTACTGGGAAAAGATATCCTGGAAATGTTTACTATTAGTGTAAGT
TTGGCTGTAGCAGCAATTCCTGAAGGTCTCCCCATTGTGGTCACAGTGACGCTAGCTCTT
GGTGTTATGAGAATGGTGAAGAAAAGGGCCATTGTGAAAAAGCTGCCTATTGTTGAAACT
CTGGGCTGCTGTAATGTGATTTGTTCAGATAAAACTGGAACACTGACGAAGAATGAAATG
ACTGTTACTCACATATTTACTTCAGATGGTCTGCATACTGAGGTTACTGGAGTTGGCTAT
AATCAATTTGGGGAAGTGATTGTTGATGGTGATGTTGTTCATGGATTCTATAACCCAGCT
GTTAGCAGAATTGTTGAGGCGGGCTGTGTGTGCAATGATGCTGTAATTAGAAACAATACT
CTAATGGGGAAGCCAACAGAAGGGGCCTTAATTGCTCTTGCAATGAAGATGGGTCTTGAT
GGACTTCAACAAGACTACATCAGAAAAGCTGAATACCCTTTTAGCTCTGAGCAAAAGTGG
ATGGCTGTTAAGTGTGTACACCGAACACAGCAGGACAGACCAGAGATTTGTTTTATGAAA
GGTGCTTACGAACAAGTAATTAAGTACTGTACTACATACCAGAGCAAAGGGCAGACCTTG
ACACTTACTCAGCAGCAGAGAGATGTGTACCAACAAGAGAAGGCACGCATGGGCTCAGCG
GGACTCAGAGTTCTTGCTTTGGCTTCTGGTCCTGAACTGGGACAGCTGACATTTCTTGGC
TTGGTGGGAATCATTGATCCACCTAGAACTGGTGTGAAAGAAGCTGTTACAACACTCATT
GCCTCAGGAGTATCAATAAAAATGATTACTGGAGATTCACAGGAGACTGCAGTTGCAATC
GCCAGTCGTCTGGGATTGTATTCCAAAACTTCCCAGTCAGTCTCAGGAGAAGAAATAGAT
GCAATGGATGTTCAGCAGCTTTCACAAATAGTACCAAAGGTTGCAGTATTTTACAGAGCT
AGCCCAAGGCACAAGATGAAAATTATTAAGTCGCTACAGAAGAACGGTTCAGTTGTAGCC
ATGACAGGAGATGGAGTAAATGATGCAGTTGCTCTGAAGGCTGCAGACATTGGAGTTGCG
ATGGGCCAGACTGGTACAGATGTTTGCAAAGAGGCAGCAGACATGATCCTAGTGGATGAT
GATTTTCAAACCATAATGTCTGCAATCGAAGAGGGTAAAGGGATTTATAATAACATTAAA
AATTTCGTTAGATTCCAGCTGAGCACGAGTATAGCAGCATTAACTTTAATCTCATTGGCT
ACATTAATGAACTTTCCTAATCCTCTCAATGCCATGCAGATTTTGTGGATCAATATTATT
ATGGATGGACCCCCAGCTCAGAGCCTTGGAGTAGAACCAGTGGATAAAGATGTCATTCGT
AAACCTCCTCGCAACTGGAAAGACAGCATTTTGACTAAAAACTTGATACTTAAAATACTT
GTTTCATCAATAATCATTGTTTGTGGGACTTTGTTTGTCTTCTGGCGTGAGCTACGAGAC
AATGTGATTACACCTCGAGACACAACAATGACCTTCACATGCTTTGTGTTTTTTGACATG
TTCAATGCACTAAGTTCCAGATCCCAGACCAAGTCTGTGTTTGAGATTGGACTCTGCAGT
AATAGAATGTTTTGCTATGCAGTTCTTGGATCCATCATGGGACAATTACTAGTTATTTAC
TTTCCTCCGCTTCAGAAGGTTTTTCAGACTGAGAGCCTAAGCATACTGGATCTGTTGTTT
CTTTTGGGTCTCACCTCATCAGTGTGCATAGTGGCAGAAATTATAAAGAAGGTTGAAAGG
AGCAGGGAAAAGATCCAGAAGCATGTTAGTTCGACATCATCATCTTTTCTTGAAGTATGA
Target 1 GenBank Gene ID
Target 1 GeneCard ID ATP2C1 Link Image
Target 1 GenAtlas ID ATP2C1 Link Image
Target 1 HGNC ID HGNC:13211 Link Image
Target 1 Chromosome Location 3
Target 1 Locus 3q22.1
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Hu Z, Bonifas JM, Beech J, Bench G, Shigihara T, Ogawa H, Ikeda S, Mauro T, Epstein EH Jr: Mutations in ATP2C1, encoding a calcium pump, cause Hailey-Hailey disease. Nat Genet. 2000 Jan;24(1):61-5. [PubMed Link Image]
  2. Nagase T, Kikuno R, Ishikawa KI, Hirosawa M, Ohara O: Prediction of the coding sequences of unidentified human genes. XVI. The complete sequences of 150 new cDNA clones from brain which code for large proteins in vitro. DNA Res. 2000 Feb 28;7(1):65-73. [PubMed Link Image]
  3. Sudbrak R, Brown J, Dobson-Stone C, Carter S, Ramser J, White J, Healy E, Dissanayake M, Larregue M, Perrussel M, Lehrach H, Munro CS, Strachan T, Burge S, Hovnanian A, Monaco AP: Hailey-Hailey disease is caused by mutations in ATP2C1 encoding a novel Ca(2+) pump. Hum Mol Genet. 2000 Apr 12;9(7):1131-40. [PubMed Link Image]
  4. Stanchi F, Bertocco E, Toppo S, Dioguardi R, Simionati B, Cannata N, Zimbello R, Lanfranchi G, Valle G: Characterization of 16 novel human genes showing high similarity to yeast sequences. Yeast. 2001 Jan 15;18(1):69-80. [PubMed Link Image]
  5. Fairclough RJ, Dode L, Vanoevelen J, Andersen JP, Missiaen L, Raeymaekers L, Wuytack F, Hovnanian A: Effect of Hailey-Hailey Disease mutations on the function of a new variant of human secretory pathway Ca2+/Mn2+-ATPase (hSPCA1). J Biol Chem. 2003 Jul 4;278(27):24721-30. Epub 2003 Apr 21. [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 482
Target 2 Name Glycine receptor subunit alpha-1
Target 2 Synonyms
  1. Glycine receptor 48 kDa subunit
  2. Glycine receptor strychnine-binding subunit
  3. Glycine receptor subunit alpha-1 precursor
Target 2 Gene Name GLRA1
Target 2 Protein Sequence >Glycine receptor subunit alpha-1 precursor 
MYSFNTLRLYLWETIVFFSLAASKEAEAARSAPKPMSPSDFLDKLMGRTSGYDARIRPNF
KGPPVNVSCNIFINSFGSIAETTMDYRVNIFLRQQWNDPRLAYNEYPDDSLDLDPSMLDS
IWKPDLFFANEKGAHFHEITTDNKLLRISRNGNVLYSIRITLTLACPMDLKNFPMDVQTC
IMQLESFGYTMNDLIFEWQEQGAVQVADGLTLPQFILKEEKDLRYCTKHYNTGKFTCIEA
RFHLERQMGYYLIQMYIPSLLIVILSWISFWINMDAAPARVGLGITTVLTMTTQSSGSRA
SLPKVSYVKAIDIWMAVCLLFVFSALLEYAAVNFVSRQHKELLRFRRKRRHHKSPMLNLF
QEDEAGEGRFNFSAYGMGPACLQAKDGISVKGANNSNTTNPPPAPSKSPEEMRKLFIQRA
KKIDKISRIGFPMAFLIFNMFYWIIYKIVRREDVHNQ
Target 2 Number of Residues 464
Target 2 Molecular Weight 52625
Target 2 Theoretical pI 9.04
Target 2 GO Classification
Function
neurotransmitter receptor activity
anion channel activity
chloride channel activity
glycine-gated chloride channel activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
GABA receptor activity
GABA-A receptor activity
Process
anion transport
inorganic anion transport
chloride transport
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 2 General Function Involved in GABA-A receptor activity
Target 2 Specific Function The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing)
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • 1-28
Target 2 Transmembrane Regions
  • 248-274
  • 281-298
  • 313-336
  • 429-446
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 31851 Link Image
Target 2 UniProtKB/Swiss-Prot ID P23415 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name GLRA1_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 2 Gene Sequence >1350 bp 
ATGTACAGCTTCAATACTCTTCGACTCTACCTTTCGGGAGCCATTGTATTCTTCAGCCTT
GCTGCTTCTAAGGAGGCTGAAGCTGCTCGCTCCGCAACCAAGCCTATGTCACCCTCGGAT
TTCCTGGATAAGCTAATGGGGAGAACCTCCGGATATGATGCCAGGATCAGGCCCAATTTT
AAAGGTCCCCCAGTGAACGTGAGCTGCAACATTTTCATCAACAGCTTTGGTTCCATTGCT
GAGACAACCATGGACTATAGGGTCAACATCTTCCTGCGGCAGCAATGGAACGACCCCCGC
CTGGCCTATAATGAATACCCTGACGACTCTCTGGACCTGGACCCATCCATGCTGGACTCC
ATCTGGAAACCTGACCTGTTCTTTGCCAACGAGAAGGGGGCCCACTTCCATGAGATCACC
ACAGACAACAAATTGCTAAGGATCTCCCGGAATGGGAATGTCCTCTACAGCATCAGAATC
ACCCTGACACTGGCCTGCCCCATGGACTTGAAGAATTTCCCCATGGATGTCCAGACATGT
ATCATGCAACTGGAAAGCTTTGGATATACGATGAATGACCTCATCTTTGAGTGGCAGGAA
CAGGGAGCCGTGCAGGTAGCAGATGGACTAACTCTGCCCCAGTTTATCTTGAAGGAAGAG
AAGGACTTGAGATACTGCACCAAGCACTACAACACAGGTAAATTCACCTGCATTGAGGCC
CGGTTCCACCTGGAGCGGCAGATGGGTTACTACCTGATTCAGATGTATATTCCCAGCCTG
CTCATTGTCATCCTCTCATGGATCTCCTTCTGGATCAACATGGATGCTGCACCTGCTCGT
GTGGGCCTAGGCATCACCACTGTGCTCACCATGACCACCCAGAGCTCCGGCTCTCGAGCA
TCTCTGCCCAAGGTGTCCTATGTGAAAGCCATTGACATTTGGATGGCAGTTTGCCTGCTC
TTTGTGTTCTCAGCCCTATTAGAATATGCTGCCGTTAACTTTGTGTCTCGGCAACATAAG
GAGCTGCTCCGATTCAGGAGGAAGCGGAGACATCACAAGGAGGATGAAGCTGGAGAAGGC
CGCTTTAACTTCTCTGCCTATGGGATGGGCCCAGCCTGTCTACAGGCCAAGGATGGCATC
TCAGTCAAGGGCGCCAACAACAGTAACACCACCAACCCCCCTCCTGCACCATCTAAGTCC
CCAGAGGAGATGCGAAAACTCTTCATCCAGAGGGCCAAGAAGATCGACAAAATATCCCGC
ATTGGCTTCCCCATGGCCTTCCTCATTTTCAACATGTTCTACTGGATCATCTACAAGATT
GTCCGTAGAGAGGACGTCCACAACCAGTGA
Target 2 GenBank Gene ID
Target 2 GeneCard ID GLRA1 Link Image
Target 2 GenAtlas ID GLRA1 Link Image
Target 2 HGNC ID HGNC:4326 Link Image
Target 2 Chromosome Location 5
Target 2 Locus 5q32
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Vergouwe MN, Tijssen MA, Peters AC, Wielaard R, Frants RR: Hyperekplexia phenotype due to compound heterozygosity for GLRA1 gene mutations. Ann Neurol. 1999 Oct;46(4):634-8. [PubMed Link Image]
  2. Grenningloh G, Schmieden V, Schofield PR, Seeburg PH, Siddique T, Mohandas TK, Becker CM, Betz H: Alpha subunit variants of the human glycine receptor: primary structures, functional expression and chromosomal localization of the corresponding genes. EMBO J. 1990 Mar;9(3):771-6. [PubMed Link Image]
  3. Shiang R, Ryan SG, Zhu YZ, Fielder TJ, Allen RJ, Fryer A, Yamashita S, O'Connell P, Wasmuth JJ: Mutational analysis of familial and sporadic hyperekplexia. Ann Neurol. 1995 Jul;38(1):85-91. [PubMed Link Image]
  4. Rees MI, Andrew M, Jawad S, Owen MJ: Evidence for recessive as well as dominant forms of startle disease (hyperekplexia) caused by mutations in the alpha 1 subunit of the inhibitory glycine receptor. Hum Mol Genet. 1994 Dec;3(12):2175-9. [PubMed Link Image]
  5. Langosch D, Laube B, Rundstrom N, Schmieden V, Bormann J, Betz H: Decreased agonist affinity and chloride conductance of mutant glycine receptors associated with human hereditary hyperekplexia. EMBO J. 1994 Sep 15;13(18):4223-8. [PubMed Link Image]
  6. Schorderet DF, Pescia G, Bernasconi A, Regli F: An additional family with Startle disease and a G1192A mutation at the alpha 1 subunit of the inhibitory glycine receptor gene. Hum Mol Genet. 1994 Jul;3(7):1201. [PubMed Link Image]
  7. Shiang R, Ryan SG, Zhu YZ, Hahn AF, O'Connell P, Wasmuth JJ: Mutations in the alpha 1 subunit of the inhibitory glycine receptor cause the dominant neurologic disorder, hyperekplexia. Nat Genet. 1993 Dec;5(4):351-8. [PubMed Link Image]
  8. Milani N, Dalpra L, del Prete A, Zanini R, Larizza L: A novel mutation (Gln266-->His) in the alpha 1 subunit of the inhibitory glycine-receptor gene (GLRA1) in hereditary hyperekplexia. Am J Hum Genet. 1996 Feb;58(2):420-2. [PubMed Link Image]
  9. Elmslie FV, Hutchings SM, Spencer V, Curtis A, Covanis T, Gardiner RM, Rees M: Analysis of GLRA1 in hereditary and sporadic hyperekplexia: a novel mutation in a family cosegregating for hyperekplexia and spastic paraparesis. J Med Genet. 1996 May;33(5):435-6. [PubMed Link Image]
  10. Seri M, Bolino A, Galietta LJ, Lerone M, Silengo M, Romeo G: Startle disease in an Italian family by mutation (K276E): The alpha-subunit of the inhibiting glycine receptor. Hum Mutat. 1997;9(2):185-7. [PubMed Link Image]
  11. 9920650 Saul B, Kuner T, Sobetzko D, Brune W, Hanefeld F, Meinck HM, Becker CM: Novel GLRA1 missense mutation (P250T) in dominant hyperekplexia defines an intracellular determinant of glycine receptor channel gating. J Neurosci. 1999 Feb 1;19(3):869-77.
Target 2 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 3 [top]
Target 3 ID 537
Target 3 Name ATP synthase delta chain, mitochondrial
Target 3 Synonyms
  1. ATP synthase delta chain, mitochondrial precursor
  2. EC 3.6.3.14
Target 3 Gene Name ATP5D
Target 3 Protein Sequence >ATP synthase delta chain, mitochondrial precursor 
MLPAALLRRPGLGRLVRHARAYAEAAAAPAAASGPNQMSFTFASPTQVFFNGANVRQVDV
PTLTGAFGILAAHVPTLQVLRPGLVVVHAEDGTTSKYFVSSGSIAVNADSSVQLLAEEAV
TLDMLDLGAAKANLEKAQAELVGTADEATRAEIQIRIEANEALVKALE
Target 3 Number of Residues 170
Target 3 Molecular Weight 17490
Target 3 Theoretical pI 5.19
Target 3 GO Classification
Function
hydrogen-transporting ATPase activity, rotational mechanism
transporter activity
ion transporter activity
cation transporter activity
monovalent inorganic cation transporter activity
hydrogen ion transporter activity
hydrogen-transporting ATP synthase activity, rotational mechanism
Process
physiological process
metabolism
cellular metabolism
cofactor metabolism
coenzyme metabolism
group transfer coenzyme metabolism
nucleoside phosphate metabolism
ATP biosynthesis
ATP synthesis coupled proton transport
Component
cell
membrane
intrinsic to membrane
integral to membrane
proton-transporting two-sector ATPase complex
Target 3 General Function Energy production and conversion
Target 3 Specific Function Produces ATP from ADP in the presence of a proton gradient across the membrane
Target 3 Pathways
Name SMPDB Link KEGG Link
ATP synthesis map00193 Link Image
Flagellar assembly map02040 Link Image
Oxidative phosphorylation map00190 Link Image
Photosynthesis map00195 Link Image
Type III secretion system map03070 Link Image
Target 3 Reactions
  • ATP + H2O + H+in = ADP + phosphate + H+out
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • None
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 12586 Link Image
Target 3 UniProtKB/Swiss-Prot ID P30049 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name ATPD_HUMAN Link Image
Target 3 PDB ID 1E79 Link Image
Target 3 PDB File Show
Target 3 3D Structure
Target 3 Cellular Location
  • Mitochondrion
Target 3 Gene Sequence >507 bp 
ATGCTGCCCGCCGCGCTGCTCCGCCGCCCGGGACTTGGCCGCCTCGTCCGCCACGCCCGT
GCCTATGCCGAGGCCGCCGCCGCCCCGGCTGCCGCCTCTGGCCCCAACCAGATGTCCTTC
ACCTTCGCCTCTCCCACGCAGGTGTTCTTCAACGGTGCCAACGTCCGGCAGGTGGACGTG
CCCACGCTGACCGGAGCCTTCGGCATCCTGGCGGCCCACGTGCCCACGCTGCAGGTCCTG
CGGCCGGGGCTGGTCGTGGTGCATGCAGAGGACGGCACCACCTCCAAATACTTTGTGAGC
AGCGGTTCCATCGCAGTGAACGCCGACTCTTCGGTGCAGTTGTTGGCCGAAGAGGCCGTG
ACGCTGGACATGTTGGACCTGGGGGCAGCCAAGGCAAACTTGGAGAAGGCCCAGGCGGAG
CTGGTGGGGACAGCTGACGAGGCCACGCGGGCAGAGATCCAGATCCGAATCGAGGCCAAC
GAGGCCCTGGTGAAGGCCCTGGAGTAG
Target 3 GenBank Gene ID
Target 3 GeneCard ID ATP5D Link Image
Target 3 GenAtlas ID ATP5D Link Image
Target 3 HGNC ID HGNC:837 Link Image
Target 3 Chromosome Location 19
Target 3 Locus 19p13.3
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Hochstrasser DF, Frutiger S, Paquet N, Bairoch A, Ravier F, Pasquali C, Sanchez JC, Tissot JD, Bjellqvist B, Vargas R, et al.: Human liver protein map: a reference database established by microsequencing and gel comparison. Electrophoresis. 1992 Dec;13(12):992-1001. [PubMed Link Image]
  2. Jordan EM, Breen GA: Molecular cloning of an import precursor of the delta-subunit of the human mitochondrial ATP synthase complex. Biochim Biophys Acta. 1992 Feb 28;1130(1):123-6. [PubMed Link Image]
Target 3 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 4 [top]
Target 4 ID 559
Target 4 Name NADH-ubiquinone oxidoreductase chain 1
Target 4 Synonyms
  1. EC 1.6.5.3
  2. NADH dehydrogenase subunit 1
Target 4 Gene Name MT-ND1
Target 4 Protein Sequence >NADH-ubiquinone oxidoreductase chain 1 
MPMANLLLLIVPILIAMAFLMLTERKILGYMQLRKGPNVVGPYGLLQPFADAMKLFTKEP
LKPATSTITLYITAPTLALTIALLLWTPLPMPNPLVNLNLGLLFILATSSLAVYSILWSG
WASNSNYALIGALRAVAQTISYEVTLAIILLSTLLMSGSFNLSTLITTQEHLWLLLPSWP
LAMMWFISTLAETNRTPFDLAEGESELVSGFNIEYAAGPFALFFMAEYTNIIMMNTLTTT
IFLGTTYDALSPELYTTYFVTKTLLLTSLFLWIRTAYPRFRYDQLMHLLWKNFLPLTLAL
LMWYVSMPITISSIPPQT
Target 4 Number of Residues 323
Target 4 Molecular Weight 35661
Target 4 Theoretical pI 6.53
Target 4 GO Classification
Function
Not Available
Process
metabolism
cellular metabolism
generation of precursor metabolites and energy
electron transport
physiological process
cellular physiological process
transport
Component
cell
membrane
Target 4 General Function Energy production and conversion
Target 4 Specific Function Not Available
Target 4 Pathways
Name SMPDB Link KEGG Link
Oxidative phosphorylation map00190 Link Image
Ubiquinone biosynthesis SMP00065 Link Image map00130 Link Image
Target 4 Reactions
  • NADH + H+ + ubiquinone = NAD+ + ubiquinol
Target 4 Pfam Domain Function
Target 4 Signals
  • None
Target 4 Transmembrane Regions
  • 4-23; 68-90; 100-122; 135-157; 172-191; 222-244; 254-273; 293-315
Target 4 Essentiality Non-Essential
Target 4 GenBank ID Protein 13004 Link Image
Target 4 UniProtKB/Swiss-Prot ID P03886 Link Image
Target 4 UniProtKB/Swiss-Prot Entry Name NU1M_HUMAN Link Image
Target 4 PDB ID Not Available
Target 4 Cellular Location
  • Mitochondrion
  • mitochondrial inner membrane
  • multi-pass membrane protein (Probable)
Target 4 Gene Sequence >957 bp 
ATACCCATGGCCAACCTCCTACTCCTCATTGTACCCATTCTAATCGCAATGGCATTCCTA
ATGCTTACCGAACGAAAAATTCTAGGCTATATACAACTACGCAAAGGCCCCAACGTGGTA
GGCCCCTACGGGCTACTACAACCCTTCGCTGACGCCATAAAACTCTTCACCAAAGAGCCC
CTAAAACCCGCCACATCTACCATCACCCTCTACATCACCGCCCCGACCTTAGCTCTCACC
ATCGCTCTTCTACTATGAACCCCCCTCCCCATACCCAACCCCCTGGTCAACCTCAACCTA
GGCCTCCTATTTATTCTAGCCACCTCTAGCCTAGCCGTTTACTCAATCCTCTGATCAGGG
TGAGCATCAAACTCAAACTACGCCCTGATCGGCGCACTGCGAGCAGTAGCCCAAACAATC
TCATATGAAGTCACCCTAGCCATCATTCTACTATCAACATTACTAATAAGTGGCTCCTTT
AACCTCTCCACCCTTATCACAACACAAGAACACCTCTGATTACTCCTGCCATCATGACCC
TTGGCCATAATATGATTTATCTCCACACTAGCAGAGACCAACCGAACCCCCTTCGACCTT
GCCGAAGGGGAGTCCGAACTAGTCTCAGGCTTCAACATCGAATACGCCGCAGGCCCCTTC
GCCCTATTCTTCATAGCCGAATACACAAACATTATTATAATAAACACCCTCACCACTACA
ATCTTCCTAGGAACAACATATGACGCACTCTCCCCTGAACTCTACACAACATATTTTGTC
ACCAAGACCCTACTTCTAACCTCCCTGTTCTTATGAATTCGAACAGCATACCCCCGATTC
CGCTACGACCAACTCATACACCTCCTATGAAAAAACTTCCTACCACTCACCCTAGCATTA
CTTATATGATATGTCTCCATACCCATTACAATCTCCAGCATTCCCCCTCAAACCTAA
Target 4 GenBank Gene ID
Target 4 GeneCard ID MT-ND1 Link Image
Target 4 GenAtlas ID MT-ND1 Link Image
Target 4 HGNC ID HGNC:7455 Link Image
Target 4 Chromosome Location MT
Target 4 Locus -
Target 4 SNPs SNPJam Report Link Image
Target 4 General References
  1. Ingman M, Kaessmann H, Paabo S, Gyllensten U: Mitochondrial genome variation and the origin of modern humans. Nature. 2000 Dec 7;408(6813):708-13. [PubMed Link Image]
  2. Ingman M, Gyllensten U: Mitochondrial genome variation and evolutionary history of Australian and New Guinean aborigines. Genome Res. 2003 Jul;13(7):1600-6. [PubMed Link Image]
  3. Johns DR, Neufeld MJ, Park RD: An ND-6 mitochondrial DNA mutation associated with Leber hereditary optic neuropathy. Biochem Biophys Res Commun. 1992 Sep 30;187(3):1551-7. [PubMed Link Image]
  4. Huoponen K, Vilkki J, Aula P, Nikoskelainen EK, Savontaus ML: A new mtDNA mutation associated with Leber hereditary optic neuroretinopathy. Am J Hum Genet. 1991 Jun;48(6):1147-53. [PubMed Link Image]
  5. Marzuki S, Noer AS, Lertrit P, Thyagarajan D, Kapsa R, Utthanaphol P, Byrne E: Normal variants of human mitochondrial DNA and translation products: the building of a reference data base. Hum Genet. 1991 Dec;88(2):139-45. [PubMed Link Image]
  6. Johns DR, Berman J: Alternative, simultaneous complex I mitochondrial DNA mutations in Leber's hereditary optic neuropathy. Biochem Biophys Res Commun. 1991 Feb 14;174(3):1324-30. [PubMed Link Image]
  7. Howell N, Bindoff LA, McCullough DA, Kubacka I, Poulton J, Mackey D, Taylor L, Turnbull DM: Leber hereditary optic neuropathy: identification of the same mitochondrial ND1 mutation in six pedigrees. Am J Hum Genet. 1991 Nov;49(5):939-50. [PubMed Link Image]
  8. Majander A, Huoponen K, Savontaus ML, Nikoskelainen E, Wikstrom M: Electron transfer properties of NADH:ubiquinone reductase in the ND1/3460 and the ND4/11778 mutations of the Leber hereditary optic neuroretinopathy (LHON). FEBS Lett. 1991 Nov 4;292(1-2):289-92. [PubMed Link Image]
  9. Howell N, Kubacka I, Xu M, McCullough DA: Leber hereditary optic neuropathy: involvement of the mitochondrial ND1 gene and evidence for an intragenic suppressor mutation. Am J Hum Genet. 1991 May;48(5):935-42. [PubMed Link Image]
  10. Chomyn A, Mariottini P, Cleeter MW, Ragan CI, Matsuno-Yagi A, Hatefi Y, Doolittle RF, Attardi G: Six unidentified reading frames of human mitochondrial DNA encode components of the respiratory-chain NADH dehydrogenase. Nature. 1985 Apr 18-24;314(6012):592-7. [PubMed Link Image]
  11. 6260957 Sanger F, Coulson AR, Barrell BG, Smith AJ, Roe BA: Cloning in single-stranded bacteriophage as an aid to rapid DNA sequencing. J Mol Biol. 1980 Oct 25;143(2):161-78.
  12. 7219534 Anderson S, Bankier AT, Barrell BG, de Bruijn MH, Coulson AR, Drouin J, Eperon IC, Nierlich DP, Roe BA, Sanger F, Schreier PH, Smith AJ, Staden R, Young IG: Sequence and organization of the human mitochondrial genome. Nature. 1981 Apr 9;290(5806):457-65.
  13. 7530363 Horai S, Hayasaka K, Kondo R, Tsugane K, Takahata N: Recent African origin of modern humans revealed by complete sequences of hominoid mitochondrial DNAs. Proc Natl Acad Sci U S A. 1995 Jan 17;92(2):532-6.
  14. 7733935 Nakagawa Y, Ikegami H, Yamato E, Takekawa K, Fujisawa T, Hamada Y, Ueda H, Uchigata Y, Miki T, Kumahara Y, et al.: A new mitochondrial DNA mutation associated with non-insulin-dependent diabetes mellitus. Biochem Biophys Res Commun. 1995 Apr 17;209(2):664-8.
  15. 8104867 Shoffner JM, Brown MD, Torroni A, Lott MT, Cabell MF, Mirra SS, Beal MF, Yang CC, Gearing M, Salvo R, et al.: Mitochondrial DNA variants observed in Alzheimer disease and Parkinson disease patients. Genomics. 1993 Jul;17(1):171-84.
  16. 8723687 Jaksch M, Hofmann S, Kaufhold P, Obermaier-Kusser B, Zierz S, Gerbitz KD: A novel combination of mitochondrial tRNA and ND1 gene mutations in a syndrome with MELAS, cardiomyopathy, and diabetes mellitus. Hum Mutat. 1996;7(4):358-60.
Target 4 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 5 [top]
Target 5 ID 705
Target 5 Name Glutamate receptor 1
Target 5 Synonyms
  1. AMPA-selective glutamate receptor 1
  2. GluR-1
  3. GluR-A
  4. GluR-K1
  5. Glutamate receptor 1 precursor
  6. Glutamate receptor ionotropic, AMPA 1
Target 5 Gene Name GRIA1
Target 5 Protein Sequence >Glutamate receptor 1 precursor 
MQHIFAFFCTGFLGAVVGANFPNNIQIGGLFPNQQSQEHAAFRFALSQLTEPPKLLPQID
IVNISDSFEMTYRFCSQFSKGVYAIFGFYERRTVNMLTSFCGALHVCFITPSFPVDTSNQ
FVLQLRPELQDALISIIDHYKWQKFVYIYDADRGLSVLQKVLDTAAEKNWQVTAVNILTT
TEEGYRMLFQDLEKKKERLVVVDCESERLNAILGQIIKLEKNGIGYHYILANLGFMDIDL
NKFKESGANVTGFQLVNYTDTIPAKIMQQWKNSDARDHTRVDWKRPKYTSALTYDGVKVM
AEAFQSLRRQRIDISRRGNAGDCLANPAVPWGQGIDIQRALQQVRFEGLTGNVQFNEKGR
RTNYTLHVIEMKHDGIRKIGYWNEDDKFVPAATDAQAGGDNSSVQNRTYIVTTILEDPYV
MLKKNANQFEGNDRYEGYCVELAAEIAKHVGYSYRLEIVSDGKYGARDPDTKAWNGMVGE
LVYGRADVAVAPLTITLVREEVIDFSKPFMSLGISIMIKKPQKSKPGVFSFLDPLAYEIW
MCIVFAYIGVSVVLFLVSRFSPYEWHSEEFEEGRDQTTSDQSNEFGIFNSLWFSLGAFMQ
QGCDISPRSLSGRIVGGVWWFFTLIIISSYTANLAAFLTVERMVSPIESAEDLAKQTEIA
YGTLEAGSTKEFFRRSKIAVFEKMWTYMKSAEPSVFVRTTEEGMIRVRKSKGKYAYLLES
TMNEYIEQRKPCDTMKVGGNLDSKGYGIATPKGSALRNPVNLAVLKLNEQGLLDKLKNKW
WYDKGECGSGGGDSKDKTSALSLSNVAGVFYILIGGLGLAMLVALIEFCYKSRSESKRMK
GFCLIPQQSINEAIRTSTLPRNSGAGASSGGSGENGRVVSHDFPKSMQSIPCMSHSSGMP
LGATGL
Target 5 Number of Residues 921
Target 5 Molecular Weight 101507
Target 5 Theoretical pI 7.78
Target 5 GO Classification
Function
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
excitatory extracellular ligand-gated ion channel activity
glutamate-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
glutamate receptor activity
ionotropic glutamate receptor activity
Process
physiological process
cellular physiological process
transport
ion transport
Component
cell
membrane
Target 5 General Function Involved in ionotropic glutamate receptor activity
Target 5 Specific Function L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. The postsynaptic actions of Glu are mediated by a variety of receptors that are named according to their selective agonists
Target 5 Pathways Not Available
Target 5 Reactions Not Available
Target 5 Pfam Domain Function
Target 5 Signals
  • 1-18
Target 5 Transmembrane Regions
  • 537-557
  • 585-605
  • 618-638
  • 806-826
Target 5 Essentiality Non-Essential
Target 5 GenBank ID Protein 183281 Link Image
Target 5 UniProtKB/Swiss-Prot ID P42261 Link Image
Target 5 UniProtKB/Swiss-Prot Entry Name GRIA1_HUMAN Link Image
Target 5 PDB ID 1WVJ Link Image
Target 5 PDB File Show
Target 5 3D Structure
Target 5 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 5 Gene Sequence >2724 bp 
ATGCAGCACATTTTTGCCTTCTTCTGCACCGGTTTCCTAGGCGCGGTAGTAGGTGCCAAT
TTCCCCAACAATATCCAGATCGGGGGATTATTTCCAAACCAGCAGTCACAGGAACATGCT
GCTTTTAGATTTGCTTTGTCGCAACTCACAGAGCCCCCGAAGCTGCTCCCCCAGATTGAT
ATTGTGAACATCAGCGACAGCTTTGAGATGACCTATAGATTCTGTTCCCAGTTCTCCAAA
GGAGTCTATGCCATCTTTGGGTTTTATGAACGTAGGACTGTCAACATGCTGACCTCCTTT
TGTGGGGCCCTCCACGTCTGCTTCATTACGCCGAGCTTTCCCGTTGATACATCCAATCAG
TTTGTCCTTCAGCTGCGCCCTGAACTGCAGGATGCCCTCATCAGCATCATTGACCATTAC
AAGTGGCAGAAATTTGTCTACATTTATGATGCCGACCGGGGCTTATCCGTCCTGCAGAAA
GTCCTGGATACAGCTGCTGAGAAGAACTGGCAGGTGACAGCAGTCAACATCTTGACAACC
ACAGAGGAGGGATACCGGATGCTCTTTCAGGACCTGGAGAAGAAAAAGGAGCGGCTGGTG
GTGGTGGACTGTGAATCAGAACGCCTCAATGCTATCTTGGGCCAGATTATAAAGCTAGAG
AAGAATGGCATCGGCTACCACTACATTCTTGCAAATCTGGGCTTCATGGACATTGACTTA
AACAAATTCAAGGAGAGTGGCGCCAATGTGACAGGTTTCCAGCTGGTGAACTACACAGAC
ACTATTCCGGCCAAGATCATGCAGCAGTGGAAGAATAGTGATGCTCGAGACCACACACGG
GTGGACTGGAAGAGACCCAAGTACACCTCTGCGCTCACCTACGATGGGGTGAAGGTGATG
GCTGAGGCTTTCCAGAGCCTGCGGAGGCAGAGAATTGATATATCTCGCCGGGGGAATGCT
GGGGATTGTCTGGCTAACCCAGCTGTTCCCTGGGGCCAAGGGATCGACATCCAGAGAGCT
CTGCAGCAGGTGCGATTTGAAGGTTTAACAGGAAACGTGCAGTTTAATGAGAAAGGACGC
CGGACCAACTACACGCTCCACGTGATTGAAATGAAACATGACGGCATCCGAAAGATTGGT
TACTGGAATGAAGATGATAAGTTTGTCCCTGCAGCCACCGATGCCCAAGCTGGGGGCGAT
AATTCAAGTGTTCAGAACAGAACATACATCGTCACAACAATCCTAGAAGATCCTTATGTG
ATGCTCAAGAAGAACGCCAATCAGTTTGAGGGCAATGACCGTTACGAGGGCTACTGTGTA
GAGCTGGCGGCAGAGATTGCCAAGCACGTGGGCTACTCCTACCGTCTGGAGATTGTCAGT
GATGGAAAATACGGAGCCCGAGACCCTGACACGAAGGCCTGGAATGGCATGGTGGGAGAG
CTGGTCTATGGAAGAGCAGATGTGGCTGTGGCTCCCTTAACTATCACTTTGGTCCGGGAA
GAAGTTATAGATTTCTCCAAACCATTTATGAGTTTGGGGATCTCCATCATGATTAAAAAA
CCACAGAAATCCAAGCCGGGTGTCTTCTCCTTCCTTGATCCTTTGGCTTATGAGATTTGG
ATGTGCATTGTTTTTGCCTACATTGGAGTGAGTGTTGTCCTCTTCCTGGTCAGCCGCTTC
AGTCCCTATGAATGGCACAGTGAAGAGTTTGAGGAAGGACGGGACCAGACAACCAGTGAC
CAGTCCAATGAGTTTGGGATATTCAACAGTTTGTGGTTCTCCCTGGGAGCCTTCATGCAG
CAAGGATGTGACATTTCTCCCAGGTCCCTGTCTGGTCGCATCGTTGGTGGCGTCTGGTGG
TTCTTCACCTTAATCATCATCTCCTCATATACAGCCAATCTGGCCGCCTTCCTGACCGTG
GAGAGGATGGTGTCTCCCATTGAGAGTGCAGAGGACCTAGCGAAGCAGACAGAAATTGCC
TACGGGACGCTGGAAGCAGGATCTACTAAGGAGTTCTTCAGGAGGTCTAAAATTGCTGTG
TTTGAGAAGATGTGGACATACATGAAGTCAGCAGAGCCATCAGTTTTTGTGCGGACCACA
GAGGAGGGGATGATTCGAGTGAGGAAATCCAAAGGCAAATATGCCTACCTCCTGGAGTCC
ACCATGAATGAGTACATTGAGCAGCGGAAACCCTGTGACACCATGAAGGTGGGAGGTAAC
TTGGATTCCAAAGGCTATGGCATTGCAACACCCAAGGGGTCTGCCCTGAGAGGTCCCGTA
AACCTAGCGGTTTTGAAACTCAGTGAGCAAGGCGTCTTAGACAAGCTGAAAAGCAAATGG
TGGTACGATAAAGGGGAATGTGGAAGCAAGGACTCCGGAAGTAAGGACAAGACAAGCGCT
CTGAGCCTCAGCAATGTGGCAGGCGTGTTCTACATCCTGATCGGAGGACTTGGACTAGCC
ATGCTGGTTGCCTTAATCGAGTTCTGCTACAAATCCCGTAGTGAATCCAAGCGGATGAAG
GGTTTTTGTTTGATCCCACAGCAATCCATCAACGAAGCCATACGGACATCGACCCTCCCC
CGCAACAGCGCGGGCACGGCACCGAGCAGCGGCGGCAGTGGAGAGAATGGTCGGGTGGTC
AGCCATGACTTCCCCAAGTCCATGCAATCGATTCCTTGCATGAGCCACAGTTCAGGGATG
CCCTTGGGAGCCACGGGATTGTAA
Target 5 GenBank Gene ID
Target 5 GeneCard ID GRIA1 Link Image
Target 5 GenAtlas ID GRIA1 Link Image
Target 5 HGNC ID HGNC:4571 Link Image
Target 5 Chromosome Location 5
Target 5 Locus 5q33|5q31.1
Target 5 SNPs SNPJam Report Link Image
Target 5 General References
  1. Sun W, Ferrer-Montiel AV, Schinder AF, McPherson JP, Evans GA, Montal M: Molecular cloning, chromosomal mapping, and functional expression of human brain glutamate receptors. Proc Natl Acad Sci U S A. 1992 Feb 15;89(4):1443-7. [PubMed Link Image]
  2. Potier MC, Spillantini MG, Carter NP: The human glutamate receptor cDNA GluR1: cloning, sequencing, expression and localization to chromosome 5. DNA Seq. 1992;2(4):211-8. [PubMed Link Image]
  3. Puckett C, Gomez CM, Korenberg JR, Tung H, Meier TJ, Chen XN, Hood L: Molecular cloning and chromosomal localization of one of the human glutamate receptor genes. Proc Natl Acad Sci U S A. 1991 Sep 1;88(17):7557-61. [PubMed Link Image]
Target 5 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 6 [top]
Target 6 ID 858
Target 6 Name Potassium voltage-gated channel subfamily A member 1
Target 6 Synonyms
  1. HBK1
  2. HUKI
  3. Voltage-gated potassium channel subunit Kv1.1
Target 6 Gene Name KCNA1
Target 6 Protein Sequence >Potassium voltage-gated channel subfamily A member 1 
MTVMSGENVDEASAAPGHPQDGSYPRQADHDDHECCERVVINISGLRFETQLKTLAQFPN
TLLGNPKKRMRYFDPLRNEYFFDRNRPSFDAILYYYQSGGRLRRPVNVPLDMFSEEIKFY
ELGEEAMEKFREDEGFIKEEERPLPEKEYQRQVWLLFEYPESSGPARVIAIVSVMVILIS
IVIFCLETLPELKDDKDFTGTVHRIDNTTVIYNSNIFTDPFFIVETLCIIWFSFELVVRF
FACPSKTDFFKNIMNFIDIVAIIPYFITLGTEIAEQEGNQKGEQATSLAILRVIRLVRVF
RIFKLSRHSKGLQILGQTLKASMRELGLLIFFLFIGVILFSSAVYFAEAEEAESHFSSIP
DAFWWAVVSMTTVGYGDMYPVTIGGKIVGSLCAIAGVLTIALPVPVIVSNFNYFYHRETE
GEEQAQLLHVSSPNLASDSDLSRRSSSTMSKYEYMEIEEDMNNSIAHYRQVNIRTANCTT
ANQNCVNKSKLLTDV
Target 6 Number of Residues 503
Target 6 Molecular Weight 56542
Target 6 Theoretical pI 4.82
Target 6 GO Classification
Function
voltage-gated ion channel activity
voltage-gated potassium channel activity
transporter activity
ion transporter activity
ion channel activity
binding
protein binding
Process
cation transport
monovalent inorganic cation transport
potassium ion transport
physiological process
cellular physiological process
transport
ion transport
Component
protein complex
voltage-gated potassium channel complex
cell
membrane
Target 6 General Function Inorganic ion transport and metabolism
Target 6 Specific Function Mediates the voltage-dependent potassium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a potassium-selective channel through which potassium ions may pass in accordance with their electrochemical gradient
Target 6 Pathways Not Available
Target 6 Reactions Not Available
Target 6 Pfam Domain Function
Target 6 Signals
  • None
Target 6 Transmembrane Regions
  • 168-186
  • 221-242
  • 254-274
  • 290-309
  • 326-345
  • 387-408
Target 6 Essentiality Non-Essential
Target 6 GenBank ID Protein 186663 Link Image
Target 6 UniProtKB/Swiss-Prot ID Q09470 Link Image
Target 6 UniProtKB/Swiss-Prot Entry Name KCNA1_HUMAN Link Image
Target 6 PDB ID 1EXB Link Image
Target 6 PDB File Show
Target 6 3D Structure
Target 6 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 6 Gene Sequence >1488 bp 
ATGACGGTGATGTCTGGGGAGAACGTGGACGAGGCTTCGGCCGCCCCGGGCCACCCCCAG
GATGGCAGCTACCCCCGCCAGGCCGACCACGACGACCACGAGTGCTGCGAGCGCGTGGTG
ATCAACATCTCCGGGCTGCGCTTCGAGACGCAGCTCAAGACCCTGGCGCAGTTCCCCAAC
ACGCTGCTGGGCAACCCTAAGAAACGCATGCGCTACTTCGACCCCCTGAGGAACGAGTAC
TTCTTCGACCGCAACCGGCCCAGCTTCGACGCCATCCTCTACTACTACCAGTCCGGCGGC
CGCCTGCGGAGGCCGGTCAACGTGCCCCTGGACATGTTCTCCGAGGAGATCAAGTTTTAC
GAGTTGGGCGAGGAGGCCATGGAGAAGTTCCGGGAGGACGAGGGCTTCATCAAGGAGGAG
GAGCGCCCTCTGCCCGAGAAGGAGTACCAGCGCCAGGTGTGGCTGCTCTTCGAGTACCCC
GAGAGCTCGGGGCCCGCCAGGGTCATCGCCATCGTCTCCGTCATGGTCATCCTCATCTCC
ATCGTCATCTTTTGCCTGGAGACGCTCCCCGAGCTGAAGGATGACAAGGACTTCACGGGC
ACCGTCCACCGCATCGACAACACCACGGTCATCTACAATTCCAACATCTTCACAGACCCC
TTCTTCATCGTGGAAACGCTGTGCATCATCTGGTTCTCCTTCGAGCTGGTGGTGCGCTTC
TTCGCCTGCCCCAGCAAGACGGACTTCTTCAAAAACATCATGAACTTCATAGACATTGTG
GCCATCATTCCTTATTTCATCACCCTGGGCACCGAGATAGCTGAGCAGGAAGGAAACCAG
AAGGGCGAGCAGGCCACCTCCCTGGCCATCCTCAGGGTCATCCGCTTGGTAAGGGTTTTT
AGAATCTTCAAGCTCTCCCGCCACTCTAAGGGCCTCCAGATCCTGGGCCAGACCCTCAAA
GCTAGTATGAGAGAGCTAGGGCTGCTCATCTTTTTCCTCTTCATCGGGGTCATCCTGTTT
TCTAGTGCAGTGTACTTTGCCGAGGCGGAAGAAGCTGAGTCGCACTTCTCCAGTATCCCC
GATGCTTTCTGGTGGGCGGTGGTGTCCATGACCACTGTAGGATACGGTGACATGTACCCT
GTGACAATTGGAGGCAAGATCGTGGGCTCCTTGTGTGCCATCGCTGGTGTGCTAACAATT
GCCCTGCCCGTACCTGTCATTGTGTCCAATTTCAACTATTTCTACCACCGAGAAACTGAG
GGGGAAGAGCAGGCTCAGTTGCTCCACGTCAGTTCCCCTAACTTAGCCTCTGACAGTGAC
CTCAGTCGCCGCAGTTCCTCTACTATGAGCAAGTATGAGTACATGGAGATCGAAGAGGAT
ATGAATAATAGCATAGCCCATTATAGACAGGTCAATATCAGAACTGCCAATTGCACCACA
GCTAACCAAAACTGCGTTAATAAGAGCAAGCTACTGACCGATGTTTAA
Target 6 GenBank Gene ID
Target 6 GeneCard ID KCNA1 Link Image
Target 6 GenAtlas ID KCNA1 Link Image
Target 6 HGNC ID HGNC:6218 Link Image
Target 6 Chromosome Location 12
Target 6 Locus 12p13
Target 6 SNPs SNPJam Report Link Image
Target 6 General References
  1. Hoopengardner B, Bhalla T, Staber C, Reenan R: Nervous system targets of RNA editing identified by comparative genomics. Science. 2003 Aug 8;301(5634):832-6. [PubMed Link Image]
  2. Browne DL, Gancher ST, Nutt JG, Brunt ER, Smith EA, Kramer P, Litt M: Episodic ataxia/myokymia syndrome is associated with point mutations in the human potassium channel gene, KCNA1. Nat Genet. 1994 Oct;8(2):136-40. [PubMed Link Image]
  3. Scheffer H, Brunt ER, Mol GJ, van der Vlies P, Stulp RP, Verlind E, Mantel G, Averyanov YN, Hofstra RM, Buys CH: Three novel KCNA1 mutations in episodic ataxia type I families. Hum Genet. 1998 Apr;102(4):464-6. [PubMed Link Image]
Target 6 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 7 [top]
Target 7 ID 872
Target 7 Name Gamma-aminobutyric-acid receptor subunit alpha-1
Target 7 Synonyms
  1. Gamma-aminobutyric-acid receptor subunit alpha-1 precursor
Target 7 Gene Name GABRA1
Target 7 Protein Sequence >Gamma-aminobutyric-acid receptor subunit alpha-1 precursor 
MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPG
LGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHAC
PLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVM
TTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDP
LIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKID
RLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
Target 7 Number of Residues 463
Target 7 Molecular Weight 51802
Target 7 Theoretical pI 9.61
Target 7 GO Classification
Function
neurotransmitter receptor activity
transporter activity
ion transporter activity
ion channel activity
ligand-gated ion channel activity
extracellular ligand-gated ion channel activity
signal transducer activity
receptor activity
transmembrane receptor activity
GABA receptor activity
GABA-A receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
gamma-aminobutyric acid signaling pathway
anion transport
inorganic anion transport
chloride transport
physiological process
cellular physiological process
transport
ion transport
Component
postsynaptic membrane
cell
membrane
intrinsic to membrane
integral to membrane
Target 7 General Function Involved in GABA-A receptor activity
Target 7 Specific Function GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel
Target 7 Pathways Not Available
Target 7 Reactions Not Available
Target 7 Pfam Domain Function
Target 7 Signals
  • 1-27
Target 7 Transmembrane Regions
  • 252-273
  • 279-300
  • 313-334
  • 422-443
Target 7 Essentiality Non-Essential
Target 7 GenBank ID Protein 31631 Link Image
Target 7 UniProtKB/Swiss-Prot ID P14867 Link Image
Target 7 UniProtKB/Swiss-Prot Entry Name GBRA1_HUMAN Link Image
Target 7 PDB ID Not Available
Target 7 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 7 Gene Sequence >1371 bp 
ATGAGGAAAAGTCCAGGTCTGTCTGACTGTCTTTGGGCCTGGATCCTCCTTCTGAGCACA
CTGACTGGAAGAAGCTATGGACAGCCGTCATTACAAGATGAACTTAAAGACAATACCACT
GTCTTCACCAGGATTTTGGACAGACTCCTAGATGGTTATGACAATCGCCTGAGACCAGGA
TTGGGAGAGCGTGTAACCGAAGTGAAGACTGATATCTTCGTCACCAGTTTCGGACCCGTT
TCAGACCATGATATGGAATATACAATAGATGTATTTTTCCGTCAAAGCTGGAAGGATGAA
AGGTTAAAATTTAAAGGACCTATGACAGTCCTCCGGTTAAATAACCTAATGGCAAGTAAA
ATCTGGACTCCGGACACATTTTTCCACAATGGAAAGAAGTCAGTGGCCCACAACATGACC
ATGCCCAACAAACTCCTGCGGATCACAGAGGATGGCACCTTGCTGTACACCATGAGGCTG
ACAGTGAGAGCTGAATGTCCGATGCATTTGGAGGACTTCCCTATGGATGCCCATGCTTGC
CCACTAAAATTTGGAAGTTATGCTTATACAAGAGCAGAAGTTGTTTATGAATGGACCAGA
GAGCCAGCACGCTCAGTGGTTGTAGCAGAAGATGGATCACGTCTAAACCAGTATGACCTT
CTTGGACAAACAGTAGACTCTGGAATTGTCCAGTCAAGTACAGGAGAATATGTTGTTATG
ACCACTCATTTCCACTTGAAGAGAAAGATTGGCTACTTTGTTATTCAAACATACCTGCCA
TGCATAATGACAGTGATTCTCTCACAAGTCTCCTTCTGGCTCAACAGAGAGTCTGTACCA
GCAAGAACTGTCTTTGGAGTAACAACTGTGCTCACCATGACAACATTGAGCATCAGTGCC
AGAAACTCCCTCCCTAAGGTGGCTTATGCAACAGCTATGGATTGGTTTATTGCCGTGTGC
TATGCCTTTGTGTTCTCAGCTCTGATTGAGTTTGCCACAGTAAACTATTTCACTAAGAGA
GGTTATGCATGGGATGGCAAAAGTGTGGTTCCAGAAAAGCCAAAGAAAGTAAAGGATCCT
CTTATTAAGAAAAACAACACTTACGCTCCAACAGCAACCAGCTACACCCCTAATTTGGCC
AGGGGCGACCCGGGCTTAGCCACCATTGCTAAAAGTGCAACCATAGAACCTAAAGAGGTC
AAGCCCGAAACAAAACCACCAGAACCCAAGAAAACCTTTAACAGTGTCAGCAAAATTGAC
CGACTGTCAAGAATAGCCTTCCCGCTGCTATTTGGAATCTTTAACTTAGTCTACTGGGCT
ACGTATTTAAACAGAGAGCCTCAGCTAAAAGCCCCCACACCACATCAATAG
Target 7 GenBank Gene ID
Target 7 GeneCard ID GABRA1 Link Image
Target 7 GenAtlas ID GABRA1 Link Image
Target 7 HGNC ID HGNC:4075 Link Image
Target 7 Chromosome Location 5
Target 7 Locus 5q34-q35
Target 7 SNPs SNPJam Report Link Image
Target 7 General References
  1. Cossette P, Liu L, Brisebois K, Dong H, Lortie A, Vanasse M, Saint-Hilaire JM, Carmant L, Verner A, Lu WY, Wang YT, Rouleau GA: Mutation of GABRA1 in an autosomal dominant form of juvenile myoclonic epilepsy. Nat Genet. 2002 Jun;31(2):184-9. Epub 2002 May 6. [PubMed Link Image]
  2. Schofield PR, Pritchett DB, Sontheimer H, Kettenmann H, Seeburg PH: Sequence and expression of human GABAA receptor alpha 1 and beta 1 subunits. FEBS Lett. 1989 Feb 27;244(2):361-4. [PubMed Link Image]
  3. Garrett KM, Duman RS, Saito N, Blume AJ, Vitek MP, Tallman JF: Isolation of a cDNA clone for the alpha subunit of the human GABA-A receptor. Biochem Biophys Res Commun. 1988 Oct 31;156(2):1039-45. [PubMed Link Image]
Target 7 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 8 [top]
Target 8 ID 2119
Target 8 Name Cytochrome b5
Target 8 Synonyms Not Available
Target 8 Gene Name CYB5A
Target 8 Protein Sequence >Cytochrome b5 
MAEQSDEAVKYYTLEEIQKHNHSKSTWLILHHKVYDLTKFLEEHPGGEEVLREQAGGDAT
ENFEDVGHSTDAREMSKTFIIGELHPDDRPKLNKPPETLITTIDSSSSWWTNWVIPAISA
VAVALMYRLYMAED
Target 8 Number of Residues 136
Target 8 Molecular Weight 15330
Target 8 Theoretical pI 4.61
Target 8 GO Classification Not Available
Target 8 General Function Involved in heme binding
Target 8 Specific Function Cytochrome b5 is a membrane bound hemoprotein which function as an electron carrier for several membrane bound oxygenases
Target 8 Pathways Not Available
Target 8 Reactions Not Available
Target 8 Pfam Domain Function
Target 8 Signals
  • None
Target 8 Transmembrane Regions
  • None
Target 8 Essentiality Non-Essential
Target 8 GenBank ID Protein 181227 Link Image
Target 8 UniProtKB/Swiss-Prot ID P00167 Link Image
Target 8 UniProtKB/Swiss-Prot Entry Name CYB5_HUMAN Link Image
Target 8 PDB ID 1HKO Link Image
Target 8 PDB File Show
Target 8 3D Structure
Target 8 Cellular Location
  • Isoform 1:Microsome
  • microsomal membrane
  • peripheral membrane protein. Isoform 2:Cytoplasm. Note=Bou
Target 8 Gene Sequence >405 bp 
ATGGCAGAGCAGTCGGACGAGGCCGTGAAGTACTACACCCTAGAGGAGATTCAGAAGCAC
AACCACAGCAAGAGCACCTGGCTGATCCTGCACCACAAGGTGTACGATTTGACCAAATTT
CTGGAAGAGCATCCTGGTGGGGAAGAAGTTTTAAGGGAACAAGCTGGAGGTGACGCTACT
GAGAACTTTGAGGATGTCGGGCACTCTACAGATGCCAGGGAAATGTCCAAAACATTCATC
ATTGGGGAGCTCCATCCAGATGACAGACCAAAGTTAAACAAGCCTCCGGAAACTCTTATC
ACTACTATTGATTCTAGTTCCAGTTGGTGGACCAACTGGGTGATCCCTGCCATCTCTGCA
GTGGCCGTCGCCTTGATGTATCGCCTATACATGGCAGAGGACTGA
Target 8 GenBank Gene ID
Target 8 GeneCard ID CYB5A Link Image
Target 8 GenAtlas ID CYB5A Link Image
Target 8 HGNC ID HGNC:2570 Link Image
Target 8 Chromosome Location 18
Target 8 Locus 18q23
Target 8 SNPs SNPJam Report Link Image
Target 8 General References
  1. Giordano SJ, Steggles AW: The human liver and reticulocyte cytochrome b5 mRNAs are products from a single gene. Biochem Biophys Res Commun. 1991 Jul 15;178(1):38-44. [PubMed Link Image]
  2. Ozols J: Structure of cytochrome b5 and its topology in the microsomal membrane. Biochim Biophys Acta. 1989 Jul 27;997(1-2):121-30. [PubMed Link Image]
  3. Yoo M, Steggles AW: The complete nucleotide sequence of human liver cytochrome b5 mRNA. Biochem Biophys Res Commun. 1988 Oct 14;156(1):576-80. [PubMed Link Image]
  4. Abe K, Kimura S, Kizawa R, Anan FK, Sugita Y: Amino acid sequences of cytochrome b5 from human, porcine, and bovine erythrocytes and comparison with liver microsomal cytochrome b5. J Biochem (Tokyo). 1985 Jun;97(6):1659-68. [PubMed Link Image]
  5. Rashid MA, Hagihara B, Kobayashi M, Tani S, Tsugita A: Structural studies of cytochrome b5. 3. Sequential studies on human liver cytochrome b5. J Biochem (Tokyo). 1973 Nov;74(5):985-1002. [PubMed Link Image]
  6. Nobrega FG, Ozols J: Amino acid sequences of tryptic peptides of cytochromes b5 from microsomes of human, monkey, porcine, and chicken liver. J Biol Chem. 1971 Mar 25;246(6):1706-17. [PubMed Link Image]
  7. Ozols J: Cytochrome b 5 from a normal human liver. Isolation and the partial amino acid sequence. J Biol Chem. 1972 Apr 10;247(7):2242-5. [PubMed Link Image]
Target 8 Drug References
  1. Zhang H, Myshkin E, Waskell L: Role of cytochrome b5 in catalysis by cytochrome P450 2B4. Biochem Biophys Res Commun. 2005 Dec 9;338(1):499-506. Epub 2005 Sep 15. [PubMed Link Image]
  2. Waskell L, Canova-Davis E, Philpot R, Parandoush Z, Chiang JY: Identification of the enzymes catalyzing metabolism of methoxyflurane. Drug Metab Dispos. 1986 Nov-Dec;14(6):643-8. [PubMed Link Image]
  3. Lipka JJ, Waskell LA: Methoxyflurane acts at the substrate binding site of cytochrome P450 LM2 to induce a dependence on cytochrome b5. Arch Biochem Biophys. 1989 Jan;268(1):152-60. [PubMed Link Image]
  4. Canova-Davis E, Chiang JY, Waskell L: Obligatory role of cytochrome b5 in the microsomal metabolism of methoxyflurane. Biochem Pharmacol. 1985 Jun 1;34(11):1907-12. [PubMed Link Image]
  5. Canova-Davis E, Waskell L: The identification of the heat-stable microsomal protein required for methoxyflurane metabolism as cytochrome b5. J Biol Chem. 1984 Feb 25;259(4):2541-6. [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.