IUPHAR/BPS Guide to Pharmacology CITE
https://doi.org/10.2218/gtopdb/F11/2019.4

Calcitonin receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database



Debbie Hay1, David R. Poyner2 and Christopher S. Walker1
  1. University of Auckland, New Zealand
  2. Aston University, UK


Abstract

This receptor family comprises a group of receptors for the calcitonin/CGRP family of peptides. The calcitonin (CT), amylin (AMY), calcitonin gene-related peptide (CGRP) and adrenomedullin (AM) receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on CGRP, AM, AMY, and CT receptors [122, 67]) are generated by the genes CALCR (which codes for the CT receptor) 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 proteins), 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 the CT receptor; these in turn produce variants of the AMY receptor [122], some of which can be potently activated by CGRP. The endogenous agonists are the peptides calcitonin, α-CGRP (formerly known as CGRP-I), β-CGRP (formerly known as CGRP-II), amylin (occasionally called islet-amyloid polypeptide, diabetes-associated polypeptide), adrenomedullin and adrenomedullin 2/intermedin. 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 CT receptor but it is not expressed in humans [87]. olcegepant (also known as BIBN4096BS, pKi~10.5) and telcagepant (also known as MK0974, pKi~9) are the most selective antagonists available, showing selectivity for CGRP receptors, with a particular preference for those of primate origin. CLR (calcitonin receptor-like receptor) by itself binds no known endogenous ligand, but in the presence of RAMPs it gives receptors for CGRP, adrenomedullin and adrenomedullin 2/intermedin.

Contents

This is a citation summary for Calcitonin receptors in the Guide to Pharmacology database (GtoPdb). It exists purely as an adjunct to the database to facilitate the recognition of citations to and from the database by citation analyzers. Readers will almost certainly want to visit the relevant sections of the database which are given here under database links.

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Please note that the database version for the citations given in GtoPdb are to the most recent preceding version in which the family or its subfamilies and targets were substantially changed. The links below are to the current version. If you need to consult the cited version, rather than the most recent version, please contact the GtoPdb curators.

Database links

Calcitonin receptors
http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=11
Introduction to Calcitonin receptors
http://www.guidetopharmacology.org/GRAC/FamilyIntroductionForward?familyId=11
    Receptors
        Complexes
            AMY1 receptor
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=44
            AMY2 receptor
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=45
            AMY3 receptor
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=46
            CGRP receptor
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=48
            AM1 receptor
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=49
            AM2 receptor
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=50
        Receptors and Subunits
            CT receptor
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=43
            calcitonin receptor-like receptor
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=47
        Accessory Proteins
            RAMP1
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=51
            RAMP2
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=52
            RAMP3
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=53
            RAMP1
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=51
            RAMP2
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=52
            RAMP3
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=53

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