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Showing drug card for Pegademase bovine (DB00061)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-02-19 16:03:23
Primary Accession Number DB00061
Secondary Accession Number
  • BIOD00100
  • BTD00100
Name Pegademase bovine
Drug Type
  • Approved
  • Biotech
Description Bovine adenosine deaminase derived from bovine intestine that has been extensively pegylated for extended serum half life
Synonyms
  1. Adenosine aminohydrolase
  2. Adenosine deaminase
Brand Names
  1. Adagen (Enzon Inc.)
Brand Mixtures Not Available
Chemical IUPAC Name bovine adenosine deaminase (PEGylated)
Chemical Formula C1821H2834N484O552S14
Chemical Structure Structure
Protein Sequence(s) >DB00061 sequence 
AQTPAFNKPKVELHVHLDGAIKPETILYYGRKRGIALPADTPEELQNIIGMDKPLSLPEF
LAKFDYYMPAIAGCREAVKRIAYEFVEMKAKDGVVYVEVRYSPHLLANSKVEPIPWNQAE
GDLTPDEVVSLVNQGLQEGERDFGVKVRSILCCMRHQPSWSSEVVELCKKYREQTVVAID
LAGDETIEGSSLFPGHVKAYAEAVKSGVHRTVHAGEVGSANVVKEAVDTLKTERLGHGYH
TLEDATLYNRLRQENMHFEVCPWSSYLTGAWKPDTEHPVVRFKNDQVNYSLNTDDPLIFK
STLDTDYQMTKNEMGFTEEEFKRLNINAAKSSFLPEDEKKELLDLLYKAYGMPSPASAEQ
CL
CAS Registry Number 9026-93-1
InChI Identifier Not Available
InChI Key Not Available
KEGG Drug Not Available
KEGG Compound Not Available
PubChem Compound Not Available
PubChem Substance Not Available
ChEBI ID Not Available
PharmGKB ID PA450832 Link Image
HET ID Not Available
GenBank ID AF280603 Link Image
Drug ID Number [DIN] Not Available
RxList Link http://www.rxlist.com/cgi/generic2/pegademase.htm Link Image
PDRhealth Link Not Available
Wikipedia Link Not Available
FDA Label Not Available
Material Safety Data Sheet (MSDS) Not Available
Synthesis Reference Not Available
Average Molecular Weight 40788.2000
Monoisotopic Molecular Weight Not Available
State Liquid
Melting Point MacQuarrie R, Buel E. Physical and catalytic properties of the isozymes of adenosine deaminase from human red blood cells.Mol Cell Biochem. 1982 Oct 18;48(2):121-6
Experimental Water Solubility Not Available Source: PhysProp
Predicted Water Solubility Not Available Calculated using ALOGPS
Experimental LogP/Hydrophobicity -0.428 Source: PhysProp
Predicted LogP Not Available Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS Not Available Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point 5.33
Mass Spectrum Not Available
MOL File Not Available
SDF File Not Available
PDB File Not Available
Experimental PDB ID 2BGN Link Image
Experimental PDB File Show
Experimental PDB Structure
Isomeric SMILES Not Available
Canonical SMILES Not Available
Drug Category
  • Enzyme Replacement Agents
ATC Codes Not Available
AHFS Codes Not Available
Indication For treatment of adenosine deaminase deficiency
Pharmacology Used to replace deficient or inactive adenosine deaminase which leads to severe combined immunodeficiency disease (SCID). The enzyme is responsible for converting adenosine to inosine. In the absence of adenosine deaminase, the purine substrates adenosine, 2'-deoxyadenosine and their metabolites are actually toxic to lymphocytes thereby leading to diminished immune function.
Mechanism of Action Pegademase converts adenosine (toxic) to inosine (less toxic) by deamination. It also converts 2'-deoxyadenosine to 2'-deoxyinosine via deamination.
Absorption Not Available
Toxicity Not Available
Protein Binding Not Available
Biotransformation Not Available
Half Life Not Available
Dosage Forms
Form Route
Injection, solution Intramuscular
Patient Information Not Available
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions Not Available
Food Interactions Not Available
Pathways Not Available
General References
  1. RxList Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. Adenosine kinase
Targets
  1. Adenosine A1 receptor
  2. D(1A) dopamine receptor
  3. Adenosine A2b receptor
  4. Adenosine
  5. Growth factor receptor-bound protein 2
  6. Adenosine A2a receptor
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Adenosine kinase
Enzyme 1 Gene Name ADK
Enzyme 1 SwissProt ID P55263 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >Adenosine kinase 
MAAAEEEPKPKKLKVEAPQALRENILFGMGNPLLDISAVVDKDFLDKYSLKPNDQILAED
KHKELFDELVKKFKVEYHAGGSTQNSIKVAQWMIQQPHKAATFFGCIGIDKFGEILKRKA
AEAHVDAHYYEQNEQPTGTCAACITGDNRSLIANLAAANCYKKEKHLDLEKNWMLVEKAR
VCYIAGFFLTVSPESVLKVAHHASENNRIFTLNLSAPFISQFYKESLMKVMPYVDILFGN
ETEAATFAREQGFETKDIKEIAKKTQALPKMNSKRQRIVIFTQGRDDTIMATESEVTAFA
VLDQDQKEIIDTNGAGDAFVGGFLSQLVSDKPLTECIRAGHYAASIIIRRTGCTFPEKPD
FH
Drug Target 1 [top]
Target 1 ID 16
Target 1 Name Adenosine A1 receptor
Target 1 Synonyms Not Available
Target 1 Gene Name ADORA1
Target 1 Protein Sequence >Adenosine A1 receptor 
MPPSISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVSLAVADVAVGA
LVIPLAILINIGPQTYFHTCLMVACPVLILTQSSILALLAIAVDRYLRVKIPLRYKMVVT
PRRAAVAIAGCWILSFVVGLTPMFGWNNLSAVERAWAANGSMGEPVIKCEFEKVISMEYM
VYFNFFVWVLPPLLLMVLIYLEVFYLIRKQLNKKVSASSGDPQKYYGKELKIAKSLALIL
FLFALSWLPLHILNCITLFCPSCHKPSILTYIAIFLTHGNSAMNPIVYAFRIQKFRVTFL
KIWNDHFRCQPAPPIDEDLPEERPDD
Target 1 Number of Residues 331
Target 1 Molecular Weight 36512
Target 1 Theoretical pI 8.75
Target 1 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
nucleotide receptor activity, G-protein coupled
purinergic nucleotide receptor activity, G-protein coupled
adenosine receptor activity, G-protein coupled
A1 adenosine receptor activity, G-protein coupled
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 1 General Function Involved in A1 adenosine receptor activity, G-protein coupled
Target 1 Specific Function Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 11-33
  • 47-69
  • 81-102
  • 124-146
  • 177-201
  • 236-259
  • 268-292
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 256155 Link Image
Target 1 UniProtKB/Swiss-Prot ID P30542 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name AA1R_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >981 bp 
ATGCCGCCCTCCATCTCAGCTTTCCAGGCCGCCTACATCGGCATCGAGGTGCTCATCGCC
CTGGTCTCTGTGCCCGGGAACGTGCTGGTGATCTGGGCGGTGAAGGTGAACCAGGCGCTG
CGGGATGCCACCTTCTGCTTCATCGTGTCGCTGGCGGTGGCTGATGTGGCCGTGGGTGCC
CTGGTCATCCCCCTCGCCATCCTCATCAACATTGGGCCACAGACCTACTTCCACACCTGC
CTCATGGTTGCCTGTCCGGTCCTCATCCTCACCCAGAGCTCCATCCTGGCCCTGCTGGCA
ATTGCGGTGGACCGCTACCTCCGGGTCAAGATCCCTCTCCGGTACAAGATGGTGGTGACC
CCCCGGAGGGCGGCGGTGGCCATAGCCGGCTGCTGGATCCTCTCCTTCGTGGTGGGACTG
ACCCCTATGTTTGGCTGGAACAATCTGAGTGCGGTGGAGCGGGCCTGGGCAGCCAACGGC
AGCATGGGGGAGCCCGTGATCAAGTGCGAGTTCGAGAAGGTCATCAGCATGGAGTACATG
GTCTACTTCAACTTCTTTGTGTGGGTGCTCCCCCCGCTTCTCCTCATGGTCCTCATCTAC
CTGGAGGTCTTCTACCTAATCCGCAAGCAGCTCAACAAGAAGGTGTCGGCCTCCTCCGGC
GACCCGCAGAAGTACTATGGGAAGGAGCTGAAGATCGCCAAGTCGCTGGCCCTCATCCTC
TTCCTCTTTGCCCTCAGCTGGCTGCCTTTGCACATCCTCAACTGCATCACCCTCTTCTGC
CCGTCCTGCCACAAGCCCAGCATCCTTACCTACATTGCCATCTTCCTCACGCACGGCAAC
TCGGCCATGAACCCCATTGTCTATGCCTTCCGCATCCAGAAGTTCCGCGTCACCTTCCTT
AAGATTTGGAATGACCATTTCCGCTGCCAGCCTGCACCTCCCATTGACGAGGATCTCCCA
GAAGAGAGGCCTGATGACTAG
Target 1 GenBank Gene ID
Target 1 GeneCard ID ADORA1 Link Image
Target 1 GenAtlas ID ADORA1 Link Image
Target 1 HGNC ID HGNC:262 Link Image
Target 1 Chromosome Location 1
Target 1 Locus 1q32.1
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Townsend-Nicholson A, Shine J: Molecular cloning and characterisation of a human brain A1 adenosine receptor cDNA. Brain Res Mol Brain Res. 1992 Dec;16(3-4):365-70. [PubMed Link Image]
  2. Libert F, Van Sande J, Lefort A, Czernilofsky A, Dumont JE, Vassart G, Ensinger HA, Mendla KD: Cloning and functional characterization of a human A1 adenosine receptor. Biochem Biophys Res Commun. 1992 Sep 16;187(2):919-26. [PubMed Link Image]
  3. Ren H, Stiles GL: Characterization of the human A1 adenosine receptor gene. Evidence for alternative splicing. J Biol Chem. 1994 Jan 28;269(4):3104-10. [PubMed Link Image]
Target 1 Drug References
  1. Santos PF, Caramelo OL, Carvalho AP, Duarte CB: Adenosine A1 receptors inhibit Ca2+ channels coupled to the release of ACh, but not of GABA, in cultured retina cells. Brain Res. 2000 Jan 3;852(1):10-5. [PubMed Link Image]
  2. Floreani M, Borea PA, Gessi S, Mosti L, Fossa P, Dorigo P: A new milrinone analog: role of binding to A1 adenosine receptor in its positive inotropic effect on isolated guinea pig and rat atria. J Pharmacol Exp Ther. 1997 Nov;283(2):541-7. [PubMed Link Image]
  3. Santos PF, Caramelo OL, Carvalho AP, Duarte CB: [3H]acetylcholine release from rat amacrine-like neurons is inhibited by adenosine A1 receptor activation. Neuroreport. 1998 Nov 16;9(16):3693-8. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 23
Target 2 Name D(1A) dopamine receptor
Target 2 Synonyms Not Available
Target 2 Gene Name DRD1
Target 2 Protein Sequence >D(1A) dopamine receptor 
MRTLNTSAMDGTGLVVERDFSVRILTACFLSLLILSTLLGNTLVCAAVIRFRHLRSKVTN
FFVISLAVSDLLVAVLVMPWKAVAEIAGFWPFGSFCNIWVAFDIMCSTASILNLCVISVD
RYWAISSPFRYERKMTPKAAFILISVAWTLSVLISFIPVQLSWHKAKPTSPSDGNATSLA
ETIDNCDSSLSRTYAISSSVISFYIPVAIMIVTYTRIYRIAQKQIRRIAALERAAVHAKN
CQTTTGNGKPVECSQPESSFKMSFKRETKVLKTLSVIMGVFVCCWLPFFILNCILPFCGS
GETQPFCIDSNTFDVFVWFGWANSSLNPIIYAFNADFRKAFSTLLGCYRLCPATNNAIET
VSINNNGAAMFSSHHEPRGSISKECNLVYLIPHAVGSSEDLKKEEAAGIARPLEKLSPAL
SVILDYDTDVSLEKIQPITQNGQHPT
Target 2 Number of Residues 453
Target 2 Molecular Weight 49294
Target 2 Theoretical pI 8.34
Target 2 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
amine receptor activity
dopamine receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 2 General Function Involved in dopamine receptor activity
Target 2 Specific Function This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • 24-49
  • 61-87
  • 97-119
  • 139-163
  • 193-218
  • 273-299
  • 313-337
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 30397 Link Image
Target 2 UniProtKB/Swiss-Prot ID P21728 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name DRD1_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location
  • Cell membrane
  • endoplasmic reticulum membrane
  • m
  • multi-pass membrane protein. Endoplasmic reticulum
Target 2 Gene Sequence >1341 bp 
ATGAGGACTCTGAACACCTCTGCCATGGACGGGACTGGGCTGGTGGTGGAGAGGGACTTC
TCTGTTCGTATCCTCACTGCCTGTTTCCTGTCGCTGCTCATCCTGTCCACGCTCCTGGGG
AACACGCTGGTCTGTGCTGCCGTTATCAGGTTCCGACACCTGCGGTCCAAGGTGACCAAC
TTCTTTGTCATCTCCTTGGCTGTGTCAGATCTCTTGGTGGCCGTCCTGGTCATGCCCTGG
AAGGCAGTGGCTGAGATTGCTGGCTTCTGGCCCTTTGGGTCCTTCTGTAACATCTGGGTG
GCCTTTGACATCATGTGCTCCACTGCATCCATCCTCAACCTCTGTGTGATCAGCGTGGAC
AGGTATTGGGCTATCTCCAGCCCTTTCCGGTATGAGAGAAAGATGACCCCCAAGGCAGCC
TTCATCCTGATCAGTGTGGCATGGACCTTGTCTGTACTCATCTCCTTCATCCCAGTGCAG
CTCAGCTGGCACAAGGCAAAACCCACAAGCCCCTCTGATGGAAATGCCACTTCCCTGGCT
GAGACCATAGACAACTGTGACTCCAGCCTCAGCAGGACATATGCCATCTCATCCTCTGTA
ATAAGCTTTTACATCCCTGTGGCCATCATGATTGTCACCTACACCAGGATCTACAGGATT
GCTCAGAAACAAATACGGCGCATTGCGGCCTTGGAGAGGGCAGCAGTCCACGCCAAGAAT
TGCCAGACCACCACAGGTAATGGAAAGCCTGTCGAATGTTCTCAACCGGAAAGTTCTTTT
AAGATGTCCTTCAAAAGAGAAACTAAAGTCCTGAAGACTCTGTCGGTGATCATGGGTGTG
TTTGTGTGCTGTTGGCTACCTTTCTTCATCTTGAACTGCATTTTGCCCTTCTGTGGGTCT
GGGGAGACGCAGCCCTTCTGCATTGATTCCAACACCTTTGACGTGTTTGTGTGGTTTGGG
TGGGCTAATTCATCCTTGAACCCCATCATTTATGCCTTTAATGCTGATTTTCGGAAGGCA
TTTTCAACCCTCTTAGGATGCTACAGACTTTGCCCTGCGACGAATAATGCCATAGAGACG
GTGAGTATCAATAACAATGGGGCCGCGATGTTTTCCAGCCATCATGAGCCACGAGGCTCC
ATCTCCAAGGAGTGCAATCTGGTTTACCTGATCCCACATGCTGTGGGCTCCTCTGAGGAC
CTGAAAAAGGAGGAGGCAGCTGGCATCGCCAGACCCTTGGAGAAGCTGTCCCCAGCCCTA
TCGGTCATATTGGACTATGACACTGACGTCTCTCTGGAGAAGATCCAACCCATCACACAA
AACGGTCAGCACCCAACCTGA
Target 2 GenBank Gene ID
Target 2 GeneCard ID DRD1 Link Image
Target 2 GenAtlas ID DRD1 Link Image
Target 2 HGNC ID HGNC:3020 Link Image
Target 2 Chromosome Location 5
Target 2 Locus 5q35.1
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Jin H, Xie Z, George SR, O'Dowd BF: Palmitoylation occurs at cysteine 347 and cysteine 351 of the dopamine D(1) receptor. Eur J Pharmacol. 1999 Dec 15;386(2-3):305-12. [PubMed Link Image]
  2. Sunahara RK, Niznik HB, Weiner DM, Stormann TM, Brann MR, Kennedy JL, Gelernter JE, Rozmahel R, Yang YL, Israel Y, et al.: Human dopamine D1 receptor encoded by an intronless gene on chromosome 5. Nature. 1990 Sep 6;347(6288):80-3. [PubMed Link Image]
  3. Dearry A, Gingrich JA, Falardeau P, Fremeau RT Jr, Bates MD, Caron MG: Molecular cloning and expression of the gene for a human D1 dopamine receptor. Nature. 1990 Sep 6;347(6288):72-6. [PubMed Link Image]
  4. Zhou QY, Grandy DK, Thambi L, Kushner JA, Van Tol HH, Cone R, Pribnow D, Salon J, Bunzow JR, Civelli O: Cloning and expression of human and rat D1 dopamine receptors. Nature. 1990 Sep 6;347(6288):76-80. [PubMed Link Image]
  5. Ohara K, Ulpian C, Seeman P, Sunahara RK, Van Tol HH, Niznik HB: Schizophrenia: dopamine D1 receptor sequence is normal, but has DNA polymorphisms. Neuropsychopharmacology. 1993 Feb;8(2):131-5. [PubMed Link Image]
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 268
Target 3 Name Adenosine A2b receptor
Target 3 Synonyms Not Available
Target 3 Gene Name ADORA2B
Target 3 Protein Sequence >Adenosine A2b receptor 
MLLETQDALYVALELVIAALSVAGNVLVCAAVGTANTLQTPTNYFLVSLAAADVAVGLFA
IPFAITISLGFCTDFYGCLFLACFVLVLTQSSIFSLLAVAVDRYLAICVPLRYKSLVTGT
RARGVIAVLWVLAFGIGLTPFLGWNSKDSATNNCTEPWDGTTNESCCLVKCLFENVVPMS
YMVYFNFFGCVLPPLLIMLVIYIKIFLVACRQLQRTELMDHSRTTLQREIHAAKSLAMIV
GIFALCWLPVHAVNCVTLFQPAQGKNKPKWAMNMAILLSHANSVVNPIVYAYRNRDFRYT
FHKIISRYLLCQADVKSGNGQAGVQPALGVGL
Target 3 Number of Residues 337
Target 3 Molecular Weight 36333
Target 3 Theoretical pI 8.31
Target 3 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
nucleotide receptor activity, G-protein coupled
purinergic nucleotide receptor activity, G-protein coupled
adenosine receptor activity, G-protein coupled
A2B adenosine receptor activity, G-protein coupled
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 3 General Function Involved in A2B adenosine receptor activity, G-protein coupled
Target 3 Specific Function Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • 9-31
  • 45-67
  • 79-101
  • 122-144
  • 179-203
  • 236-259
  • 268-291
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 178150 Link Image
Target 3 UniProtKB/Swiss-Prot ID P29275 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name AA2BR_HUMAN Link Image
Target 3 PDB ID Not Available
Target 3 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 3 Gene Sequence >999 bp 
ATGCTGCTGGAGACACAGGACGCGCTGTACGTGGCGCTGGAGCTGGTCATCGCCGCGCTT
TCGGTGGCGGGCAACGTGCTGGTGTGCGCCGCGGTGGGCACGGCGAACACTCTGCAGACG
CCCACCAACTACTTCCTGGTGTCCCTGGCTGCGGCCGACGTGGCCGTGGGGCTCTTCGCC
ATCCCCTTTGCCATCACCATCAGCCTGGGCTTCTGCACTGACTTCTACGGCTGCCTCTTC
CTCGCCTGCTTCGTGCTGGTGCTCACGCAGAGCTCCATCTTCAGCCTTCTGGCCGTGGCA
GTCGACAGATACCTGGCCATCTGTGTCCCGCTCAGGTATAAAAGTTTGGTCACGGGGACC
CGAGCAAGAGGGGTCATTGCTGTCCTCTGGGTCCTTGCCTTTGGCATCGGATTGACTCCA
TTCCTGGGGTGGAACAGTAAAGACAGTGCCACCAACAACTGCACAGAACCCTGGGATGGA
ACCACGAATGAAAGCTGCTGCCTTGTGAAGTGTCTCTTTGAGAATGTGGTCCCCATGAGC
TACATGGTATATTTCAATTTCTTTGGGTGTGTTCTGCCCCCACTGCTTATAATGCTGGTG
ATCTACATTAAGATCTTCCTGGTGGCCTGCAGGCAGCTTCAGCGCACTGAGCTGATGGAC
CACTCGAGGACCACCCTCCAGCGGGAGATCCATGCAGCCAAGTCACTGGCCATGATTGTG
GGGATTTTTGCCCTGTGCTGGTTACCTGTGCATGCTGTTAACTGTGTCACTCTTTTCCAG
CCAGCTCAGGGTAAAAATAAGCCCAAGTGGGCAATGAATATGGCCATTCTTCTGTCACAT
GCCAATTCAGTTGTCAATCCCATTGTCTATGCTTACCGGAACCGAGACTTCCGCTACACT
TTTCACAAAATTATCTCCAGGTATCTTCTCTGCCAAGCAGATGTCAAGAGTGGGAATGGT
CAGGCTGGGGTACAGCCTGCTCTCGGTGTGGGCCTATGA
Target 3 GenBank Gene ID
Target 3 GeneCard ID ADORA2B Link Image
Target 3 GenAtlas ID ADORA2B Link Image
Target 3 HGNC ID HGNC:264 Link Image
Target 3 Chromosome Location 17
Target 3 Locus 17p12-p11.2
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Pierce KD, Furlong TJ, Selbie LA, Shine J: Molecular cloning and expression of an adenosine A2b receptor from human brain. Biochem Biophys Res Commun. 1992 Aug 31;187(1):86-93. [PubMed Link Image]
  2. Jacobson MA, Johnson RG, Luneau CJ, Salvatore CA: Cloning and chromosomal localization of the human A2b adenosine receptor gene (ADORA2B) and its pseudogene. Genomics. 1995 May 20;27(2):374-6. [PubMed Link Image]
Target 3 Drug References
  1. Ohkubo S, Kumazawa K, Sagawa K, Kimura J, Matsuoka I: Beta,gamma-methylene ATP-induced cAMP formation in C6Bu-1 cells: involvement of local metabolism and subsequent stimulation of adenosine A2B receptor. J Neurochem. 2001 Feb;76(3):872-80. [PubMed Link Image]
Drug Target 4 [top]
Target 4 ID 879
Target 4 Name Adenosine
Target 4 Synonyms Not Available
Target 4 Gene Name Not Available
Target 4 Protein Sequence Not Available
Target 4 Number of Residues 0
Target 4 Molecular Weight 267.242
Target 4 Theoretical pI Not Available
Target 4 GO Classification Not Available
Target 4 General Function Not Available
Target 4 Specific Function Not Available
Target 4 Pathways Not Available
Target 4 Reactions
  • adenosine + H2O = inosine + NH3
Target 4 Pfam Domain Function Not Available
Target 4 Signals Not Available
Target 4 Transmembrane Regions Not Available
Target 4 Essentiality Non-Essential
Target 4 GenBank ID Protein Not Available
Target 4 UniProtKB/Swiss-Prot ID Not Available
Target 4 UniProtKB/Swiss-Prot Entry Name Not Available
Target 4 PDB ID Not Available
Target 4 Cellular Location Not Available
Target 4 Gene Sequence Not Available
Target 4 GenBank Gene ID
Target 4 GeneCard ID Not Available
Target 4 GenAtlas ID Not Available
Target 4 HGNC ID Not Available
Target 4 Chromosome Location Not Available
Target 4 Locus Not Available
Target 4 SNPs Not Available
Target 4 General References Not Available
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]
  3. Kemeny-Beke A, Jakab A, Zsuga J, Vecsernyes M, Karsai D, Pasztor F, Grenczer M, Szentmiklosi AJ, Berta A, Gesztelyi R: Adenosine deaminase inhibition enhances the inotropic response mediated by A(1) adenosine receptor in hyperthyroid guinea pig atrium. Pharmacol Res. 2007 Aug;56(2):124-31. Epub 2007 May 10. [PubMed Link Image]
  4. Mohsenin A, Mi T, Xia Y, Kellems RE, Chen JF, Blackburn MR: Genetic removal of the A2A adenosine receptor enhances pulmonary inflammation, mucin production, and angiogenesis in adenosine deaminase-deficient mice. Am J Physiol Lung Cell Mol Physiol. 2007 Sep;293(3):L753-61. Epub 2007 Jun 29. [PubMed Link Image]
  5. Van Linden A, Eltzschig HK: Role of pulmonary adenosine during hypoxia: extracellular generation, signaling and metabolism by surface adenosine deaminase/CD26. Expert Opin Biol Ther. 2007 Sep;7(9):1437-47. [PubMed Link Image]
Drug Target 5 [top]
Target 5 ID 1157
Target 5 Name Growth factor receptor-bound protein 2
Target 5 Synonyms
  1. Adapter protein GRB2
  2. Protein Ash
  3. SH2/SH3 adapter GRB2
Target 5 Gene Name GRB2
Target 5 Protein Sequence >Growth factor receptor-bound protein 2 
MEAIAKYDFKATADDELSFKRGDILKVLNEECDQNWYKAELNGKDGFIPKNYIEMKPHPW
FFGKIPRAKAEEMLSKQRHDGAFLIRESESAPGDFSLSVKFGNDVQHFKVLRDGAGKYFL
WVVKFNSLNELVDYHRSTSVSRNQQIFLRDIEQVPQQPTYVQALFDFDPQEDGELGFRRG
DFIHVMDNSDPNWWKGACHGQTGMFPRNYVTPVNRNV
Target 5 Number of Residues 220
Target 5 Molecular Weight 25207
Target 5 Theoretical pI 6.25
Target 5 GO Classification
Function
Not Available
Process
cellular process
cell communication
signal transduction
intracellular signaling cascade
Component
Not Available
Target 5 General Function Involved in epidermal growth factor receptor binding
Target 5 Specific Function Isoform GRB3-3 does not bind to phosphorylated epidermal growth factor receptor (EGFR) but inhibits EGF-induced transactivation of a RAS-responsive element. Isoform GRB3-3 acts as a dominant negative protein over GRB2 and by suppressing proliferative signals, may trigger active programmed cell death
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 181976 Link Image
Target 5 UniProtKB/Swiss-Prot ID P62993 Link Image
Target 5 UniProtKB/Swiss-Prot Entry Name GRB2_HUMAN Link Image
Target 5 PDB ID 1GRI Link Image
Target 5 PDB File Show
Target 5 3D Structure
Target 5 Cellular Location Not Available
Target 5 Gene Sequence >654 bp 
ATGGAAGCCATCGCCAAATATGACTTCAAAGCTACTGCAGACGACGAGCTGAGCTTCAAA
AGGGGGGACATCCTCAAGGTTTTGAACGAAGAATGTGATCAGAACTGGTACAAGGCAGAG
CTTAATGGAAAAGACGGCTTCATTCCCAAGAACTACATAGAAATGAAACCACATCCGTGG
TTTTTTGGCAAAATCCCCAGAGCCAAGGCAGAAGAAATGCTTAGCAAACAGCGGCACGAT
GGGGCCTTTCTTATCCGAGAGAGTGAGAGCGCTCCTGGGGACTTCTCCCTCTCTGTCAAG
TTTGGAAACGATGTGCAGCACTTCAAGGTGCTCCGAGATGGAGCCGGGAAGTACTTCCTC
TGGGTGGTGAAGTTCAATTCTTTGAATGAGCTGGTGGATTATCACAGATCTACATCTGTC
TCCAGAAACCAGCAGATATTCCTGCGGGACATAGAACAGGTGCCACAGCAGCCGACATAC
GTCCAGGCCCTCTTTGACTTTGATCCCCAGGAGGATGGAGAGCTGGGCTTCCGCCGGGGA
GATTTTATCCATGTCATGGATAACTCAGACCCCAACTGGTGGAAAGGAGCTTGCCACGGG
CAGACCGGCATGTTTCCCCGCAATTATGTCACCCCCGTGAACCGGAACGTCTAA
Target 5 GenBank Gene ID
Target 5 GeneCard ID GRB2 Link Image
Target 5 GenAtlas ID GRB2 Link Image
Target 5 HGNC ID HGNC:4566 Link Image
Target 5 Chromosome Location 17
Target 5 Locus 17q24-q25
Target 5 SNPs SNPJam Report Link Image
Target 5 General References
  1. Bochmann H, Gehrisch S, Jaross W: The gene structure of the human growth factor bound protein GRB2. Genomics. 1999 Mar 1;56(2):203-7. [PubMed Link Image]
  2. Ettmayer P, France D, Gounarides J, Jarosinski M, Martin MS, Rondeau JM, Sabio M, Topiol S, Weidmann B, Zurini M, Bair KW: Structural and conformational requirements for high-affinity binding to the SH2 domain of Grb2(1). J Med Chem. 1999 Mar 25;42(6):971-80. [PubMed Link Image]
  3. Tan SL, Nakao H, He Y, Vijaysri S, Neddermann P, Jacobs BL, Mayer BJ, Katze MG: NS5A, a nonstructural protein of hepatitis C virus, binds growth factor receptor-bound protein 2 adaptor protein in a Src homology 3 domain/ligand-dependent manner and perturbs mitogenic signaling. Proc Natl Acad Sci U S A. 1999 May 11;96(10):5533-8. [PubMed Link Image]
  4. Furet P, Garcia-Echeverria C, Gay B, Schoepfer J, Zeller M, Rahuel J: Structure-based design, synthesis, and X-ray crystallography of a high-affinity antagonist of the Grb2-SH2 domain containing an asparagine mimetic. J Med Chem. 1999 Jul 1;42(13):2358-63. [PubMed Link Image]
  5. Schiering N, Casale E, Caccia P, Giordano P, Battistini C: Dimer formation through domain swapping in the crystal structure of the Grb2-SH2-Ac-pYVNV complex. Biochemistry. 2000 Nov 7;39(44):13376-82. [PubMed Link Image]
  6. Zhu M, Janssen E, Leung K, Zhang W: Molecular cloning of a novel gene encoding a membrane-associated adaptor protein (LAX) in lymphocyte signaling. J Biol Chem. 2002 Nov 29;277(48):46151-8. Epub 2002 Sep 30. [PubMed Link Image]
  7. Brdicka T, Imrich M, Angelisova P, Brdickova N, Horvath O, Spicka J, Hilgert I, Luskova P, Draber P, Novak P, Engels N, Wienands J, Simeoni L, Osterreicher J, Aguado E, Malissen M, Schraven B, Horejsi V: Non-T cell activation linker (NTAL): a transmembrane adaptor protein involved in immunoreceptor signaling. J Exp Med. 2002 Dec 16;196(12):1617-26. [PubMed Link Image]
  8. Janssen E, Zhu M, Zhang W, Koonpaew S, Zhang W: LAB: a new membrane-associated adaptor molecule in B cell activation. Nat Immunol. 2003 Feb;4(2):117-23. Epub 2003 Jan 6. [PubMed Link Image]
  9. Lowenstein EJ, Daly RJ, Batzer AG, Li W, Margolis B, Lammers R, Ullrich A, Skolnik EY, Bar-Sagi D, Schlessinger J: The SH2 and SH3 domain-containing protein GRB2 links receptor tyrosine kinases to ras signaling. Cell. 1992 Aug 7;70(3):431-42. [PubMed Link Image]
  10. Matuoka K, Shibata M, Yamakawa A, Takenawa T: Cloning of ASH, a ubiquitous protein composed of one Src homology region (SH) 2 and two SH3 domains, from human and rat cDNA libraries. Proc Natl Acad Sci U S A. 1992 Oct 1;89(19):9015-9. [PubMed Link Image]
  11. 7716522 Maignan S, Guilloteau JP, Fromage N, Arnoux B, Becquart J, Ducruix A: Crystal structure of the mammalian Grb2 adaptor. Science. 1995 Apr 14;268(5208):291-3.
  12. 7881903 Kohda D, Terasawa H, Ichikawa S, Ogura K, Hatanaka H, Mandiyan V, Ullrich A, Schlessinger J, Inagaki F: Solution structure and ligand-binding site of the carboxy-terminal SH3 domain of GRB2. Structure. 1994 Nov 15;2(11):1029-40.
  13. 8178156 Fath I, Schweighoffer F, Rey I, Multon MC, Boiziau J, Duchesne M, Tocque B: Cloning of a Grb2 isoform with apoptotic properties. Science. 1994 May 13;264(5161):971-4.
  14. 8388384 Tobe K, Matuoka K, Tamemoto H, Ueki K, Kaburagi Y, Asai S, Noguchi T, Matsuda M, Tanaka S, Hattori S, et al.: Insulin stimulates association of insulin receptor substrate-1 with the protein abundant Src homology/growth factor receptor-bound protein 2. J Biol Chem. 1993 May 25;268(15):11167-71.
  15. 8491186 Skolnik EY, Lee CH, Batzer A, Vicentini LM, Zhou M, Daly R, Myers MJ Jr, Backer JM, Ullrich A, White MF, et al.: The SH2/SH3 domain-containing protein GRB2 interacts with tyrosine-phosphorylated IRS1 and Shc: implications for insulin control of ras signalling. EMBO J. 1993 May;12(5):1929-36.
  16. 8794768 Thornton KH, Mueller WT, McConnell P, Zhu G, Saltiel AR, Thanabal V: Nuclear magnetic resonance solution structure of the growth factor receptor-bound protein 2 Src homology 2 domain. Biochemistry. 1996 Sep 10;35(36):11852-64.
  17. 9062191 Kharitonenkov A, Chen Z, Sures I, Wang H, Schilling J, Ullrich A: A family of proteins that inhibit signalling through tyrosine kinase receptors. Nature. 1997 Mar 13;386(6621):181-6.
  18. 9233773 Yokouchi M, Suzuki R, Masuhara M, Komiya S, Inoue A, Yoshimura A: Cloning and characterization of APS, an adaptor molecule containing PH and SH2 domains that is tyrosine phosphorylated upon B-cell receptor stimulation. Oncogene. 1997 Jul 3;15(1):7-15.
  19. 9422736 Ikeda M, Ishida O, Hinoi T, Kishida S, Kikuchi A: Identification and characterization of a novel protein interacting with Ral-binding protein 1, a putative effector protein of Ral. J Biol Chem. 1998 Jan 9;273(2):814-21.
  20. 9489702 Zhang W, Sloan-Lancaster J, Kitchen J, Trible RP, Samelson LE: LAT: the ZAP-70 tyrosine kinase substrate that links T cell receptor to cellular activation. Cell. 1998 Jan 9;92(1):83-92.
  21. 9642078 Rahuel J, Garcia-Echeverria C, Furet P, Strauss A, Caravatti G, Fretz H, Schoepfer J, Gay B: Structural basis for the high affinity of amino-aromatic SH2 phosphopeptide ligands. J Mol Biol. 1998 Jun 19;279(4):1013-22.
Target 5 Drug References
  1. Ramos-Morales F, Dominguez A, Rios RM, Barroso SI, Infante C, Schweighoffer F, Tocque B, Pintor-Toro JA, Tortolero M: Adenosine deaminase is a specific partner for the Grb2 isoform Grb3-3. Biochem Biophys Res Commun. 1997 Aug 28;237(3):735-40. [PubMed Link Image]
Drug Target 6 [top]
Target 6 ID 1178
Target 6 Name Adenosine A2a receptor
Target 6 Synonyms Not Available
Target 6 Gene Name ADORA2A
Target 6 Protein Sequence >Adenosine A2a receptor 
MPIMGSSVYITVELAIAVLAILGNVLVCWAVWLNSNLQNVTNYFVVSLAAADIAVGVLAI
PFAITISTGFCAACHGCLFIACFVLVLTQSSIFSLLAIAIDRYIAIRIPLRYNGLVTGTR
AKGIIAICWVLSFAIGLTPMLGWNNCGQPKEGKNHSQGCGEGQVACLFEDVVPMNYMVYF
NFFACVLVPLLLMLGVYLRIFLAARRQLKQMESQPLPGERARSTLQKEVHAAKSLAIIVG
LFALCWLPLHIINCFTFFCPDCSHAPLWLMYLAIVLSHTNSVVNPFIYAYRIREFRQTFR
KIIRSHVLRQQEPFKAAGTSARVLAAHGSDGEQVSLRLNGHPPGVWANGSAPHPERRPNG
YALGLVSGGSAQESQGNTGLPDVELLSHELKGVCPEPPGLDDPLAQDGAGVS
Target 6 Number of Residues 418
Target 6 Molecular Weight 44708
Target 6 Theoretical pI 8.05
Target 6 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
nucleotide receptor activity, G-protein coupled
purinergic nucleotide receptor activity, G-protein coupled
adenosine receptor activity, G-protein coupled
A2A adenosine receptor activity, G-protein coupled
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 6 General Function Involved in A2A adenosine receptor activity, G-protein coupled
Target 6 Specific Function Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase
Target 6 Pathways Not Available
Target 6 Reactions Not Available
Target 6 Pfam Domain Function
Target 6 Signals
  • None
Target 6 Transmembrane Regions
  • 8-30
  • 44-66
  • 78-100
  • 121-143
  • 174-198
  • 235-258
  • 267-290
Target 6 Essentiality Non-Essential
Target 6 GenBank ID Protein 177892 Link Image
Target 6 UniProtKB/Swiss-Prot ID P29274 Link Image
Target 6 UniProtKB/Swiss-Prot Entry Name AA2AR_HUMAN Link Image
Target 6 PDB ID Not Available
Target 6 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 6 Gene Sequence >1230 bp 
ATGGGCTCCTCGGTGTACATCACGGTGGAGCTGGCCATTGCTGTGCTGGCCATCCTGGGC
AATGTGCTGGTGTGCTGGGCCGTGTGGCTCAACAGCAACCTGCAGAACGTCACCAACTAC
TTTGTGGTGTCACTGGCGGCGGCCGACATCGCAGTGGGTGTGCTCGCCATCCCCTTTGCC
ATCACCATCAGCACCGGGTTCTGCGCTGCCTGCCACGGCTGCCTCTTCATTGCCTGCTTC
GTCCTGGTCCTCACGCAGAGCTCCATCTTCAGTCTCCTGGCCATCGCCATTGACCGCTAC
ATTGCCATCCGCATCCCGCTCCGGTACAATGGCTTGGTGACCGGCACGAGGGCTAAGGGC
ATCATTGCCATCTGCTGGGTGCTGTCGTTTGCCATCGGCCTGACTCCCATGCTAGGTTGG
AACAACTGCGGTCAGCCAAAGGAGGGCAAGAACCACTCCCAGGGCTGCGGGGAGGGCCAA
GTGGCCTGTCTCTTTGAGGATGTGGTCCCCATGAACTACATGGTGTACTTCAACTTCTTT
GCCTGTGTGCTGGTGCCCCTGCTGCTCATGCTGGGTGTCTATTTGCGGATCTTCCTGGCG
GCGCGACGACAGCTGAAGCAGATGGAGAGCCAGCCTCTGCCGGGGGAGCGGGCACGGTCC
ACACTGCAGAAGGAGGTCCATGCTGCCAAGTCACTGGCCATCATTGTGGGGCTCTTTGCC
CTCTGCTGGCTGCCCCTACACATCATCAACTGCTTCACTTTCTTCTGCCCCGACTGCAGC
CACGCCCCTCTCTGGCTCATGTACCTGGCCATCGTCCTCTCCCACACCAATTCGGTTGTG
AATCCCTTCATCTACGCCTACCGTATCCGCGAGTTCCGCCAGACCTTCCGCAAGATCATT
CGCAGCCACGTCCTGAGGCAGCAAGAACCTTTCAAGGCAGCTGGCACCAGTGCCCGGGTC
TTGGCAGCTCATGGCAGTGACGGAGAGCAGGTCAGCCTCCGTCTCAACGGCCACCCGCCA
GGAGTGTGGGCCAACGGCAGTGCTCCCCACCCTGAGCGGAGGCCCAATGGCTATGCCCTG
GGGCTGGTGAGTGGAGGGAGTGCCCAAGAGTCCCAGGGGAACACGGGCCTCCCAGACGTG
GAGCTCCTTAGCCATGAGCTCAAGGGAGTGTGCCCAGAGCCCCCTGGCCTAGATGACCCC
CTGGCCCAGGATGGAGCAGGAGTGTCCTGA
Target 6 GenBank Gene ID
Target 6 GeneCard ID ADORA2A Link Image
Target 6 GenAtlas ID ADORA2A Link Image
Target 6 HGNC ID HGNC:263 Link Image
Target 6 Chromosome Location 22
Target 6 Locus 22q11.23
Target 6 SNPs SNPJam Report Link Image
Target 6 General References
  1. Cargill M, Altshuler D, Ireland J, Sklar P, Ardlie K, Patil N, Shaw N, Lane CR, Lim EP, Kalyanaraman N, Nemesh J, Ziaugra L, Friedland L, Rolfe A, Warrington J, Lipshutz R, Daley GQ, Lander ES: Characterization of single-nucleotide polymorphisms in coding regions of human genes. Nat Genet. 1999 Jul;22(3):231-8. [PubMed Link Image]
  2. Furlong TJ, Pierce KD, Selbie LA, Shine J: Molecular characterization of a human brain adenosine A2 receptor. Brain Res Mol Brain Res. 1992 Sep;15(1-2):62-6. [PubMed Link Image]
  3. Kim J, Wess J, van Rhee AM, Schoneberg T, Jacobson KA: Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor. J Biol Chem. 1995 Jun 9;270(23):13987-97. [PubMed Link Image]
  4. Le F, Townsend-Nicholson A, Baker E, Sutherland GR, Schofield PR: Characterization and chromosomal localization of the human A2a adenosine receptor gene: ADORA2A. Biochem Biophys Res Commun. 1996 Jun 14;223(2):461-7. [PubMed Link Image]
Target 6 Drug References
  1. Inglis VI, Jones MP, Tse AD, Easton AS: Neutrophils both reduce and increase permeability in a cell culture model of the blood-brain barrier. Brain Res. 2004 Feb 20;998(2):218-29. [PubMed Link Image]
  2. Wright K, Tajouri L, Lea RA, Ovcaric M, Heux S, Morin F, Bey W, Headrick JP, Griffiths LR: The role of adenosine-related genes variants in susceptibility to essential hypertension. J Hypertens. 2004 Aug;22(8):1519-22. [PubMed Link Image]
  3. Dayton C, Yamaguchi T, Kamada K, Carter P, Korthuis RJ: Antecedent ethanol ingestion prevents postischemic P-selectin expression in murine small intestine. Microcirculation. 2004 Dec;11(8):709-18. [PubMed Link Image]
  4. Vissiennon Z, Sichardt K, Koetter U, Brattstrom A, Nieber K: Valerian extract Ze 911 inhibits postsynaptic potentials by activation of adenosine A1 receptors in rat cortical neurons. Planta Med. 2006 Jun;72(7):579-83. Epub 2006 Apr 28. [PubMed Link Image]
  5. Cartmell J, Schaffhauser H, Wichmann J, Mutel V: mGluR-evoked augmentation of receptor-mediated cyclic AMP formation in neonatal and adult rat striatum. Br J Pharmacol. 1997 Aug;121(7):1263-8. [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.