Target Information

Target General Infomation
Target ID
T32247
Former ID
TTDS00485
Target Name
Calcitonin receptor
Gene Name
CALCR
Synonyms
CT-R; CALCR
Target Type
Successful
Disease Hypertension [ICD9: 401; ICD10: I10-I16]
Osteoporosis [ICD9: 733.0, V07.4; ICD10: M80-M81, Z79.890]
Pain; Postmenopausal osteoporosis [ICD9:338, 356.0, 356.8, 780, 733; ICD10: G64, G90.0, R52, G89, M80-M81]
Paget's disease [ICD9: 731; ICD10: M88]
Function
Thisis a receptor for calcitonin. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. The calcitonin receptor is thought to couple to the heterotrimeric guanosine triphosphate-binding protein that is sensitive to cholera toxin.
BioChemical Class
GPCR secretin
Target Validation
T32247
UniProt ID
P30988
Sequence
MQFSGEKISGQRDLQKSKMRFTFTSRCLALFLLLNHPTPILPAFSNQTYPTIEPKPFLYV
VGRKKMMDAQYKCYDRMQQLPAYQGEGPYCNRTWDGWLCWDDTPAGVLSYQFCPDYFPDF
DPSEKVTKYCDEKGVWFKHPENNRTWSNYTMCNAFTPEKLKNAYVLYYLAIVGHSLSIFT
LVISLGIFVFFRKLTTIFPLNWKYRKALSLGCQRVTLHKNMFLTYILNSMIIIIHLVEVV
PNGELVRRDPVSCKILHFFHQYMMACNYFWMLCEGIYLHTLIVVAVFTEKQRLRWYYLLG
WGFPLVPTTIHAITRAVYFNDNCWLSVETHLLYIIHGPVMAALVVNFFFLLNIVRVLVTK
MRETHEAESHMYLKAVKATMILVPLLGIQFVVFPWRPSNKMLGKIYDYVMHSLIHFQGFF
VATIYCFCNNEVQTTVKRQWAQFKIQWNQRWGRRPSNRSARAAAAAAEAGDIPIYICHQE
PRNEPANNQGEESAEIIPLNIIEQESSA
Drugs and Mode of Action
Drug(s) Calcitonin Human Drug Info Approved Paget's disease [551871]
Salmon Calcitonin Drug Info Approved Osteoporosis [536361], [542004]
Calcitonin oral Drug Info Phase 3 Pain; Postmenopausal osteoporosis [531853]
TJN-220 Drug Info Terminated Hypertension [545256]
Modulator Calcitonin Human Drug Info [556264]
Calcitonin oral Drug Info [544165]
TJN-220 Drug Info [533777]
Inhibitor CGNLSTCBLGTYTQDFNKFHZYPQTAIGVGAP-amide Drug Info [526273]
CGNLSTCBLGTYTQDF[DKFHO]YPQTAIGVGAP-amide Drug Info [526273]
CGNLSTCMLGTYTQDFc[DKFHK]FPQTAIGVGAP-amide Drug Info [526273]
CGNLSTCMLGTYTQDFc[DKFHO]FPQTAIGVGAP-amide Drug Info [526273]
CGNLSTCMLGTYTQDFNKFHTFPQTAIGVGAP-amide Drug Info [526273]
CGNLSTCMLGTYTQDFNKPHTFPQTAIGVGAP-amide Drug Info [526273]
CGNLSTCMLGTYTQDFNPFHTFPQTAIGVGAP-amide Drug Info [526273]
CGNLSTCMLGTYTQDFNPKHTFPQTAIGVGAP-amide Drug Info [526273]
CSNLSTCVLGKLSQELc[DKLHK]YPRTNTGSGTP-amide Drug Info [526273]
CSNLSTCVLGKLSQELc[DKLHO]YPRTNTGSGTP-amide Drug Info [526273]
CSNLSTCVLGKLSQELc[DKLQK]YPRTNTGSGTP-amide Drug Info [526273]
CSNLSTCVLGKLSQELHKLQTYPRTNTGSGTP-amide Drug Info [526273]
CSNLSTCVLGKLSQELNKLHBYPRTNTGSGTP-amide Drug Info [526273]
Binder Salmon Calcitonin Drug Info [537494], [537723]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Osteoclast differentiation
NetPath Pathway RANKL Signaling Pathway
Reactome G alpha (s) signalling events
Calcitonin-like ligand receptors
WikiPathways GPCRs, Class B Secretin-like
RANKL/RANK Signaling Pathway
GPCR ligand binding
GPCR downstream signaling
References
Ref 531853A phase 3 trial of the efficacy and safety of oral recombinant calcitonin: the Oral Calcitonin in Postmenopausal Osteoporosis (ORACAL) trial. J Bone Miner Res. 2012 Aug;27(8):1821-9.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 542004(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6973).
Ref 545256Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002586)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 526273J Med Chem. 2002 Feb 28;45(5):1108-21.Side-chain lactam-bridge conformational constraints differentiate the activities of salmon and human calcitonins and reveal a new design concept for potent calcitonin analogues.
Ref 533777Evaluation of the long-lasting antihypertensive action of 7-O-ethylfangchinoline. Jpn J Pharmacol. 1994 Sep;66(1):35-46.
Ref 537494Improved absorption of salmon calcitonin by ultraflexible liposomes through intranasal delivery. Peptides. 2009 Jul;30(7):1288-95. Epub 2009 Apr 7.
Ref 537723Purification and characterization of calcitonin receptors in rat kidney membranes by covalent cross-linking techniques. Eur J Biochem. 1986 Feb 17;155(1):141-7.
Ref 544165Transdermal Delivery of Proteins. AAPS PharmSciTech. 2011 March; 12(1): 431-441.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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