Calcitonin receptors

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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Calcitonin (CT), amylin (AMY), calcitonin gene-related peptide (CGRP) and adrenomedullin (AM) receptors (nomenclature as agreed by NC-IUPHAR Subcommittee on CGRP, AM, AMY, and CT receptors, [12,21]) are generated by the genes CALCR (which codes for the CT receptor (CTR),) and CALCRL (which codes for the calcitonin receptor-like receptor, CLR, previously known as CRLR,). Their function and pharmacology are altered in the presence of RAMPs (receptor activity-modifying protein), which are single TM domain proteins of ca. 130 amino acids, identified as a family of three members; RAMP1, RAMP2 and RAMP3. There are splice variants of CTR; these in turn produce variants of the AMY receptor [21]. The endogenous agonists are the peptides CT (CALCA, P01258), α-CGRP (CALCA, P06881) (formerly known as CGRP-I), β-CGRP (CALCB, P10092) (formerly known as CGRP-II), AMY (IAPP, P10997) (occasionally called islet-amyloid polypeptide, diabetes-associated polypeptide), AM (ADM, P35318) and AM2/IMD (ADM2, Q7Z4H4) (AM2/IMD). There are species differences in peptide sequences, particularly for the CTs. CTR-stimulating peptide (CRSP) is another member of the family with selectivity for the CTR but it is not expressed in humans [14]. olcegepant (also known as BIBN4096BS, pKi~10.5) and telcagepant (also known as MK0974, pKi~9) are the most selective antagonists available, having a high selectivity for CGRP receptors, with a particular preference for those of primate origin.

CLR by itself binds no known endogenous ligand, but in the presence of RAMPs it gives receptors for CGRP, AM and AM2/IMD.

Receptors

AMY1 receptor Show summary » More detailed page

AMY2 receptor Show summary » More detailed page

AMY3 receptor Show summary » More detailed page

CGRP receptor Show summary » More detailed page

AM1 receptor Show summary » More detailed page

AM2 receptor Show summary » More detailed page

Subunits

CT receptor Show summary » More detailed page

calcitonin receptor-like receptor Show summary » More detailed page

Accessory proteins

RAMP1 Show summary » More detailed page

RAMP2 Show summary » More detailed page

RAMP3 Show summary » More detailed page

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References

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation:

Calcitonin receptors. Accessed on 18/09/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=11.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Spedding M, Peters JA and Harmar AJ, CGTP Collaborators. (2013) The Concise Guide to PHARMACOLOGY 2013/14: G Protein-Coupled Receptors. Br J Pharmacol. 170: 1459–1581.