Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTLWS2O)

• DTT Name: Calcitonin receptor (CALCR)
• Synonyms: CT-R
• Gene Name: CALCR
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR secretin
• UniProt ID: CALCR_HUMAN
• TTD ID: T32247
• Sequence:
  MRFTFTSRCLALFLLLNHPTPILPAFSNQTYPTIEPKPFLYVVGRKKMMDAQYKCYDRMQ
  QLPAYQGEGPYCNRTWDGWLCWDDTPAGVLSYQFCPDYFPDFDPSEKVTKYCDEKGVWFK
  HPENNRTWSNYTMCNAFTPEKLKNAYVLYYLAIVGHSLSIFTLVISLGIFVFFRSLGCQR
  VTLHKNMFLTYILNSMIIIIHLVEVVPNGELVRRDPVSCKILHFFHQYMMACNYFWMLCE
  GIYLHTLIVVAVFTEKQRLRWYYLLGWGFPLVPTTIHAITRAVYFNDNCWLSVETHLLYI
  IHGPVMAALVVNFFFLLNIVRVLVTKMRETHEAESHMYLKAVKATMILVPLLGIQFVVFP
  WRPSNKMLGKIYDYVMHSLIHFQGFFVATIYCFCNNEVQTTVKRQWAQFKIQWNQRWGRR
  PSNRSARAAAAAAEAGDIPIYICHQEPRNEPANNQGEESAEIIPLNIIEQESSA
• Function: 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. This is a receptor for calcitonin.
• KEGG Pathway:
  Neuroactive ligand-receptor interaction (hsa04080)
  Osteoclast differentiation (hsa04380)
• Reactome Pathway:
  Calcitonin-like ligand receptors (R-HSA-419812)
  G alpha (s) signalling events (R-HSA-418555)

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Calcitonin Human	DM0N9WA	Paget's disease	FB85	Approved	[2]
Salmon Calcitonin	DMEWUPF	Bone Paget disease		Approved	[1]

2 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
DACRA 089	DM5TB76	Type 2 diabetes	5A11	Phase 1	[3]
LY 3541105	DMJ1X85	Obesity	5B81	Phase 1	[4]

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
TJN-220	DM4YQDX	Hypertension	BA00-BA04	Terminated	[5]

13 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CGNLSTCBLGTYTQDFNKFHZYPQTAIGVGAP-amide	DMLA384	Discovery agent	N.A.	Investigative	[6]
CGNLSTCBLGTYTQDF[DKFHO]YPQTAIGVGAP-amide	DMQ3SAY	Discovery agent	N.A.	Investigative	[6]
CGNLSTCMLGTYTQDFc[DKFHK]FPQTAIGVGAP-amide	DMUGAYT	Discovery agent	N.A.	Investigative	[6]
CGNLSTCMLGTYTQDFc[DKFHO]FPQTAIGVGAP-amide	DM3FP47	Discovery agent	N.A.	Investigative	[6]
CGNLSTCMLGTYTQDFNKFHTFPQTAIGVGAP-amide	DMJ9Z31	Discovery agent	N.A.	Investigative	[6]
CGNLSTCMLGTYTQDFNKPHTFPQTAIGVGAP-amide	DME84PN	Discovery agent	N.A.	Investigative	[6]
CGNLSTCMLGTYTQDFNPFHTFPQTAIGVGAP-amide	DMV7TE4	Discovery agent	N.A.	Investigative	[6]
CGNLSTCMLGTYTQDFNPKHTFPQTAIGVGAP-amide	DMMO8A2	Discovery agent	N.A.	Investigative	[6]
CSNLSTCVLGKLSQELc[DKLHK]YPRTNTGSGTP-amide	DMYDTO8	Discovery agent	N.A.	Investigative	[6]
CSNLSTCVLGKLSQELc[DKLHO]YPRTNTGSGTP-amide	DMQXEHJ	Discovery agent	N.A.	Investigative	[6]
CSNLSTCVLGKLSQELc[DKLQK]YPRTNTGSGTP-amide	DMMZK89	Discovery agent	N.A.	Investigative	[6]
CSNLSTCVLGKLSQELHKLQTYPRTNTGSGTP-amide	DMTL2BA	Discovery agent	N.A.	Investigative	[6]
CSNLSTCVLGKLSQELNKLHBYPRTNTGSGTP-amide	DM61V5W	Discovery agent	N.A.	Investigative	[6]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Osteoporosis	FA20	Bone marrow	7.52E-03	0.17	2.26

References

• [1] Improved absorption of salmon calcitonin by ultraflexible liposomes through intranasal delivery. Peptides. 2009 Jul;30(7):1288-95.
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [3] A novel dual amylin and calcitonin receptor agonist, KBP-089, induces weight loss through a reduction in fat, but not lean mass, while improving food preference. Br J Pharmacol. 2017 Apr;174(7):591-602.
• [4] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight
• [5] Evaluation of the long-lasting antihypertensive action of 7-O-ethylfangchinoline. Jpn J Pharmacol. 1994 Sep;66(1):35-46.
• [6] Side-chain lactam-bridge conformational constraints differentiate the activities of salmon and human calcitonins and reveal a new design concept fo... J Med Chem. 2002 Feb 28;45(5):1108-21.