Therapeutic Targets Database
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TTD Target ID: TTDC00110

Target Information
NameHepatocyte growth factor receptor    
Type of targetSuccessful target    
SynonymsC-Met receptor tyrosine kinase    
C-met    
HGF receptor    
HGF-SF receptor    
Met proto-oncogene tyrosine kinase    
DiseaseGastric Cancer
[ICD9: 151   ICD10: C16]
[1][2]
Hepatocellular carcinoma
[ICD9: 155   ICD10: C22.0]
[3]
Lung cancer
[ICD9: 162   ICD10: C33-C34]
[4]
Pancreatic Cancer
[ICD9: 157   ICD10: C25]
[5]
Prostate cancer (metastatic)
[ICD9: 140-229, 185   ICD10: C00-C96, C61]
[6]
Renal Cell Carcinoma
[ICD9: 189   ICD10: C64]
[1][2]
Small cell lung cancer
[ICD9: 162.9   ICD10: C34.90]
[7]
Solid tumors
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[8][1][2][9]
Drug(s)CrizotinibApprovedALK-positive advanced or metastatic NSCLC
CabozantinibPhase IIIMedullary Thyroid Cancer[10]
RG3638Phase IIIMetastatic HER2-negative gastric cancer
ARQ 197Phase IISolid Tumors, Pancreatic Cancer[11]
Anti-cMetPhase IICancer[12]
CabozantinibPhase IIBreast Cancer, Gastric/GE Junctional Cancer, Hepatocellular Carcinoma, Melanoma, Castration-Resistant Prostate Cancer, Non-small Cell Lung Cancer, Ovarian Cancer, Pancreatic Cancer, Small Cell Lung Cance[10]
CabozantinibPhase IIMetastatic Castration-Resistant Prostate Cancer, Ovarian Cancer[10]
LY2801653Phase IICancer
LY2875358Phase IICancer
MetMAbPhase IIMetastatic non-small cell lung cancer[13]
RG3638Phase II1st line non-squamous non-small cell lung cancer
RG3638Phase II1st line squamous non-small cell lung cancer
RG3638Phase IIAvastin-nave recurrent glioblastoma
RG3638Phase IIMetastatic colorectal cancer
RG3638Phase IITriple negative metastatic breast cancer
XL880Phase IIGastric Cancer, Renal Cell Carcinoma, Squamous Cell Cancer of the Head and Neck[14][1][2][15][16]
INC280Phase I/IISolid Tumors
MK-8033Phase I completedAdvanced Cancer[17]
CabozantinibPhase IbDifferentiated Thyroid Cancer, Renal Cell Carcinoma[10]
ABT-700Phase ISolid Tumors
AMG 208Phase ISolid Tumors
AMG 208Phase IVarious cancer types
AMG 337Phase ISolid Tumors
AMG 337Phase IVarious cancer types
C-Met inhibitorPhase ICancer
EMD-1214063Phase ISolid Tumors
INCB28060Phase ISolid tumors
MP470Phase ISolid Tumors[8]
SAR125844Phase ISolid Tumors
SAR125844Phase ISolid tumors
TAK-701Phase IAdvanced malignancies[18]
VolitinibPhase ISolid tumours
XL880Phase ISolid Tumors[14][1][2][15][16]
SGX523Terminated in Phase ISolid Tumors[5]
Mteron-F1PreclinicalChemotherapy-induced mucositis[19]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.112
PathwayAdherens junction
Axon guidance
Colorectal cancer
Cytokine-cytokine receptor interaction
Epithelial cell signaling in Helicobacter pylori
Focal adhesion
Melanoma
Pathways in cancer
Renal cell carcinoma
UniProt IDP08581
PDB Structure1FYR; 1R0P; 1R1W; 1SHY; 1SSL; 1UX3; 2G15; 2RFN; 2RFS; 2UZX; 2UZY; 2WD1; 2WGJ; 2WKM; 3A4P; 3BUX; 3C1X; 3CCN; 3CD8; 3CE3; 3CTH; 3CTJ; 3DKC; 3DKF; 3DKG; 3EFJ; 3EFK; 3F66; 3F82; 3I5N; 3L8V; 3LQ8; 3Q6U; 3Q6W; 3QTI; 3R7O; 3RHK; 3U6H; 3U6I; 3ZXZ; 3ZZE; 4AOI; 4AP7; 4DEG; 4DEH; 4DEI; 4EEV; 4GG5; 4GG7.    
FunctionReceptor for hepatocyte growth factor. Has a tyrosine- protein kinase activity.    
SequenceMKAPAVLAPGILVLLFTLVQRSNGECKEALAKSEMNVNMKYQLPNFTAETPIQNVILHEH HIFLGATNYIYVLNEEDLQKVAEYKTGPVLEHPDCFPCQDCSSKANLSGGVWKDNINMAL VVDTYYDDQLISCGSVNRGTCQRHVFPHNHTADIQSEVHCIFSPQIEEPSQCPDCVVSAL GAKVLSSVKDRFINFFVGNTINSSYFPDHPLHSISVRRLKETKDGFMFLTDQSYIDVLPE FRDSYPIKYVHAFESNNFIYFLTVQRETLDAQTFHTRIIRFCSINSGLHSYMEMPLECIL TEKRKKRSTKKEVFNILQAAYVSKPGAQLARQIGASLNDDILFGVFAQSKPDSAEPMDRS AMCAFPIKYVNDFFNKIVNKNNVRCLQHFYGPNHEHCFNRTLLRNSSGCEARRDEYRTEF TTALQRVDLFMGQFSEVLLTSISTFIKGDLTIANLGTSEGRFMQVVVSRSGPSTPHVNFL LDSHPVSPEVIVEHTLNQNGYTLVITGKKITKIPLNGLGCRHFQSCSQCLSAPPFVQCGW CHDKCVRSEECLSGTWTQQICLPAIYKVFPNSAPLEGGTRLTICGWDFGFRRNNKFDLKK TRVLLGNESCTLTLSESTMNTLKCTVGPAMNKHFNMSIIISNGHGTTQYSTFSYVDPVIT SISPKYGPMAGGTLLTLTGNYLNSGNSRHISIGGKTCTLKSVSNSILECYTPAQTISTEF AVKLKIDLANRETSIFSYREDPIVYEIHPTKSFISGGSTITGVGKNLNSVSVPRMVINVH EAGRNFTVACQHRSNSEIICCTTPSLQQLNLQLPLKTKAFFMLDGILSKYFDLIYVHNPV FKPFEKPVMISMGNENVLEIKGNDIDPEAVKGEVLKVGNKSCENIHLHSEAVLCTVPNDL LKLNSELNIEWKQAISSTVLGKVIVQPDQNFTGLIAGVVSISTALLLLLGFFLWLKKRKQ IKDLGSELVRYDARVHTPHLDRLVSARSVSPTTEMVSNESVDYRATFPEDQFPNSSQNGS CRQVQYPLTDMSPILTSGDSDISSPLLQNTVHIDLSALNPELVQAVQHVVIGPSSLIVHF NEVIGRGHFGCVYHGTLLDNDGKKIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVL SLLGICLRSEGSPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKF VHRDLAARNCMLDEKFTVKVADFGLARDMYDKEYYSVHNKTGAKLPVKWMALESLQTQKF TTKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVMLKCW HPKAEMRPSFSELVSRISAIFSTFIGEHYVHVNATYVNVKCVAPYPSLLSSEDNADDEVD TRPASFWETS
Related US Patent6,468,529
Target ValidationClick to Find Target Validation Information.    
Inhibitor1- (2-nitrophenethyl)-1H-pyrrolo[3,2-b]pyridine[20]
1- (phenylsulfonyl)-1H-pyrrolo[3,2-b]pyridine[20]
1-benzyl-1H-pyrrolo[3,2-b]pyridine[20]
3- (phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine[20]
ARQ 197[11]
BMS-536924[21]
BMS-777607[22]
Cabozantinib[10]
K-252a[23]
MK-8033[17]
MP470[8]
SGX523[5]
XL880[14][1][2][15][16]
AntibodyAnti-cMet[12]
MetMAb[13]
TAK-701[18]
StimulatorMteron-F1[19]
MultitargetCabozantinib[10]
MP470[8]
XL880[14][1][2][15][16]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib. Proc Natl Acad Sci U S A. 2007 Dec 26;104(52):20932-7. Epub 2007 Dec 18. To Reference
Ref 2Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Mar;29(2):153-73. To Reference
Ref 3Activation of the Met receptor by cell attachment induces and sustains hepatocellular carcinomas in transgenic mice. J Cell Biol. 2001 May 28;153(5):1023-34. To Reference
Ref 4c-Met: structure, functions and potential for therapeutic inhibition. Cancer Metastasis Rev. 2003 Dec;22(4):309-25. To Reference
Ref 5CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. To Reference
Ref 6High expression of the Met receptor in prostate cancer metastasis to bone. Urology. 2002 Dec;60(6):1113-7. To Reference
Ref 7c-MET mutational analysis in small cell lung cancer: novel juxtamembrane domain mutations regulating cytoskeletal functions. Cancer Res. 2003 Oct 1;63(19):6272-81. To Reference
Ref 8MP470, a novel receptor tyrosine kinase inhibitor, in combination with Erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer. BMC Cancer. 2009 May 11;9:142. To Reference
Ref 9Oncogene. 2007 Jun 7;26(27):3909-19. Epub 2007 Feb 26.A novel tyrosine kinase switch is a mechanism of imatinib resistance in gastrointestinal stromal tumors. To Reference
Ref 102011 Pipeline of Exelixis. To Reference
Ref 11ArQule Announces Acceptance of Clinical Data on ARQ 197, c-Met Inhibitor, for Oral Presentation at ASCO. ArQule. 2008 To Reference
Ref 12Roche. Product Development Pipeline. July 29 2009. To Reference
Ref 13Genentech. Product Development Pipeline. July 2009. To Reference
Ref 14Pipeline of EXELIXIS. EXELIXIS. 2009 To Reference
Ref 152011 Pipeline of Exelixis. To Reference
Ref 16GSK. Product Development Pipeline. February 2009. To Reference
Ref 17Merck. Product Development Pipeline. July 15 2009. To Reference
Ref 18Takeda. Product Development Pipeline. July 31 2009. To Reference
Ref 19Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22. To Reference
Ref 20Bioorg Med Chem Lett. 2009 May 15;19(10):2780-4. Epub 2009 Mar 27.Discovery of 4-azaindoles as novel inhibitors of c-Met kinase. To Reference
Ref 21J Med Chem. 2005 Sep 8;48(18):5639-43.Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. To Reference
Ref 22J Med Chem. 2009 Mar 12;52(5):1251-4.Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily. To Reference
Ref 23Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference



 

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