Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00164

Target Information
NameExtracellular calcium-sensing receptor    
Type of targetSuccessful target    
SynonymsCaSR    
Parathyroid Cell calcium-sensing receptor    
Parathyroid calcium receptor    
Parathyroid cell calcium receptor    
DiseaseHyperparathyroidism, unspecified
[ICD9: 252.0   ICD10: E21]
[1]
Drug(s)CinacalcetApprovedHyperparathyroidism[2]
CinacalcetPhase IIICardiovascular disease and kidney disease[3]
AMG 416Phase IISecondary hyperparathyroidism in patients with chronic kidney disease receiving dialysis
MK-5442Phase IIOsteoporosis
RonacaleretSuspended in Phase II in GSK 2009 ReportOsteoporosis & fracture healing[4]
BioChemical ClassG-protein coupled receptor (metabotropic glutamate family)    
UniProt IDP41180
FunctionSenses changes in the extracellular concentration of calcium ions. The activity of this receptor is mediated by a G-protein that activates a phosphatidylinositol-calcium second messenger system.    
SequenceMAFYSCCWVLLALTWHTSAYGPDQRAQKKGDIILGGLFPIHFGVAAKDQDLKSRPESVEC IRYNFRGFRWLQAMIFAIEEINSSPALLPNLTLGYRIFDTCNTVSKALEATLSFVAQNKI DSLNLDEFCNCSEHIPSTIAVVGATGSGVSTAVANLLGLFYIPQVSYASSSRLLSNKNQF KSFLRTIPNDEHQATAMADIIEYFRWNWVGTIAADDDYGRPGIEKFREEAEERDICIDFS ELISQYSDEEEIQHVVEVIQNSTAKVIVVFSSGPDLEPLIKEIVRRNITGKIWLASEAWA SSSLIAMPQYFHVVGGTIGFALKAGQIPGFREFLKKVHPRKSVHNGFAKEFWEETFNCHL QEGAKGPLPVDTFLRGHEESGDRFSNSSTAFRPLCTGDENISSVETPYIDYTHLRISYNV YLAVYSIAHALQDIYTCLPGRGLFTNGSCADIKKVEAWQVLKHLRHLNFTNNMGEQVTFD ECGDLVGNYSIINWHLSPEDGSIVFKEVGYYNVYAKKGERLFINEEKILWSGFSREVPFS NCSRDCLAGTRKGIIEGEPTCCFECVECPDGEYSDETDASACNKCPDDFWSNENHTSCIA KEIEFLSWTEPFGIALTLFAVLGIFLTAFVLGVFIKFRNTPIVKATNRELSYLLLFSLLC CFSSSLFFIGEPQDWTCRLRQPAFGISFVLCISCILVKTNRVLLVFEAKIPTSFHRKWWG LNLQFLLVFLCTFMQIVICVIWLYTAPPSSYRNQELEDEIIFITCHEGSLMALGFLIGYT CLLAAICFFFAFKSRKLPENFNEAKFITFSMLIFFIVWISFIPAYASTYGKFVSAVEVIA ILAASFGLLACIFFNKIYIILFKPSRNTIEEVRCSTAAHAFKVAARATLRRSNVSRKRSS SLGGSTGSTPSSSISSKSNSEDPFPQPERQKQQQPLALTQQEQQQQPLTLPQQQRSQQQP RCKQKVIFGSGTVTFSLSFDEPQKNAMAHRNSTHQNSLEAQKSSDTLTRHQPLLPLQCGE TDLDLTVQETGLQGPVGGDQRPEVEDPEELSPALVVSSSQSFVISGGGSTVTENVVNS
Target ValidationClick to Find Target Validation Information.    
Inhibitor2-Furan-2-yl-3-phenethyl-3H-quinazolin-4-one[5]
3-Phenethyl-2-phenyl-3H-quinazolin-4-one[6]
NPS-2143,   SB-262470A[7]
AgonistAMG 073[8]
Cinacalcet[3]
Cinacalcet[2]
NPS 568[8]
R-568[1]
AntagonistRonacaleret[4]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Mixed-effects modeling of the pharmacodynamic response to the calcimimetic agent R-568. Clin Pharmacol Ther. 1999 Jan;65(1):40-9. To Reference
Ref 2Expression and function of the calcium-sensing receptor in juxtaglomerular cells. Hypertension. 2007 Oct;50(4):737-43. Epub 2007 Sep 4. To Reference
Ref 3Amgen. Product Development Pipeline. February 6 2009. To Reference
Ref 4GSK. Product Development Pipeline. February 2009. To Reference
Ref 5Bioorg Med Chem Lett. 2005 May 16;15(10):2537-40.Design, new synthesis, and calcilytic activity of substituted 3H-pyrimidin-4-ones. To Reference
Ref 6Bioorg Med Chem Lett. 2005 Mar 15;15(6):1557-60.3H-Quinazolin-4-ones as a new calcilytic template for the potential treatment of osteoporosis. To Reference
Ref 7J Med Chem. 2006 Aug 24;49(17):5119-28.N1-Benzoyl-N2-[1-(1-naphthyl)ethyl]-trans-1,2-diaminocyclohexanes: Development of 4-chlorophenylcarboxamide (calhex 231) as a new calcium sensing receptor ligand demonstrating potent calcilytic activity. To Reference
Ref 8Calcimimetics: therapeutic potential in hyperparathyroidism. Curr Opin Pharmacol. 2002 Dec;2(6):734-9. To Reference



 

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