Therapeutic Targets Database
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TTD Target ID: TTDC00344

Target Information
NameSmoothened    
Type of targetClinical trial target    
SynonymsProtein Gx    
SMO    
Smoothened homolog    
DiseaseCancers    [1]
Drug(s)BMS-833923Phase IbCancers[1]
UniProt IDQ99835
FunctionG protein-coupled receptor that probably associates with the patched protein (PTCH) to transduce the hedgehog's proteins signal. Binding of sonic hedgehog (SHH) to its receptor patched is thought to prevent normal inhibition by patched of smoothened (SMO). Required for the accumulation of KIF7 and GLI3 in the cilia.    
SequenceMAAARPARGPELPLLGLLLLLLLGDPGRGAASSGNATGPGPRSAGGSARRSAAVTGPPPP LSHCGRAAPCEPLRYNVCLGSVLPYGATSTLLAGDSDSQEEAHGKLVLWSGLRNAPRCWA VIQPLLCAVYMPKCENDRVELPSRTLCQATRGPCAIVERERGWPDFLRCTPDRFPEGCTN EVQNIKFNSSGQCEVPLVRTDNPKSWYEDVEGCGIQCQNPLFTEAEHQDMHSYIAAFGAV TGLCTLFTLATFVADWRNSNRYPAVILFYVNACFFVGSIGWLAQFMDGARREIVCRADGT MRLGEPTSNETLSCVIIFVIVYYALMAGVVWFVVLTYAWHTSFKALGTTYQPLSGKTSYF HLLTWSLPFVLTVAILAVAQVDGDSVSGICFVGYKNYRYRAGFVLAPIGLVLIVGGYFLI RGVMTLFSIKSNHPGLLSEKAASKINETMLRLGIFGFLAFGFVLITFSCHFYDFFNQAEW ERSFRDYVLCQANVTIGLPTKQPIPDCEIKNRPSLLVEKINLFAMFGTGIAMSTWVWTKA TLLIWRRTWCRLTGQSDDEPKRIKKSKMIAKAFSKRHELLQNPGQELSFSMHTVSHDGPV AGLAFDLNEPSADVSSAWAQHVTKMVARRGAILPQDISVTPVATPVPPEEQANLWLVEAE ISPELQKRLGRKKKRRKRKKEVCPLAPPPELHPPAPAPSTIPRLPQLPRQKCLVAAGAWG AGDSCRQGAWTLVSNPFCPEPSPPQDPFLPSAPAPVAWAHGRRQGLGPIHSRTNLMDTEL MDADSDF
Target ValidationClick to Find Target Validation Information.    
Inhibitor1-Benzyl-4- (4-phenylpiperazin-1-yl)phthalazine[2]
BMS-833923[1]
CYCLOPAMINE[3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 12011 Pipeline of Exelixis. To Reference
Ref 2J Med Chem. 2009 Jul 9;52(13):3954-68.1-amino-4-benzylphthalazines as orally bioavailable smoothened antagonists with antitumor activity. To Reference
Ref 3Bioorg Med Chem Lett. 2009 Jan 15;19(2):328-31. Epub 2008 Dec 3.Identification and structure-activity relationships of ortho-biphenyl carboxamides as potent Smoothened antagonists inhibiting the Hedgehog signaling pathway. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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