Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00348

Target Information
NameProto-oncogene tyrosine-protein kinase receptor ret    
Type of targetSuccessful target    
SynonymsC-ret    
RET receptor tyrosine kinase    
DiseaseMedullary thyroid carcinoma[1]
Drug(s)SorafenibLaunchedAdvanced renal cell carcinoma[2][3][4]
SorafenibPhase IIIHepatocellular carcinoma, NSCLC, melanoma[2][3][4]
VandetanibPhase IIISolid tumours, NSCLC[2][5]
SorafenibPhase IIMyelodyspalstic syndrome, AML, head & neck cancer, breast, colon, ovarian, pancreatic cancer[2][3][4]
VandetanibPhase IIBreast, thyroid tumours, multiple myeloma, brain, head & neck cancer[2][5]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.112
PathwayPathways in cancer
Thyroid cancer
UniProt IDP07949
PDB Structure1XPD; 2IVS; 2IVT; 2IVU; 2IVV; 2X2K; 2X2L; 2X2M; 2X2U.    
FunctionProbable receptor with tyrosine-protein kinase activity; Important for development.    
SequenceMAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAP EEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLT VYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENR PPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELV AVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFD ADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNR NLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFA QIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAE LHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGR CEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPR GIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCY HKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFP RKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLK QVNHPHVIKLYGACSQDGPLLLIVEYAKYGSLRGFLRESRKVGPGYLGSGGSRNSSSLDH PDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVY EEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERL FNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAA STPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRA DGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
Target ValidationClick to Find Target Validation Information.    
Inhibitor (E)-3-[6]
(Z)-3-[6]
(Z)-5-Amino-3-[6]
CEP-751[1]
SEMAXINIB[6]
SU-11248[6]
SU-4984[6]
SU-5614[6]
SU-6656[6]
SU-9516[6]
Sorafenib[2][3][4]
TG-100435[7]
Vandetanib[2][5]
MultitargetSorafenib[2][3][4]
Vandetanib[2][5]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1CEP-701 and CEP-751 inhibit constitutively activated RET tyrosine kinase activity and block medullary thyroid carcinoma cell growth. Cancer Res. 2003 Sep 1;63(17):5559-63. To Reference
Ref 2A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. To Reference
Ref 3Pituitary tumors. Curr Treat Options Neurol. 2009 Jul;11(4):287-96. To Reference
Ref 4Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42. Epub 2006 Nov 28. To Reference
Ref 5AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 6Bioorg Med Chem. 2010 Feb 15;18(4):1482-96. Epub 2010 Jan 11.Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. To Reference
Ref 7Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. Epub 2006 Nov 7.Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays. To Reference



 

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