International Union of Pharmacology. XXXII. The Mammalian Calcitonin Gene-Related Peptides, Adrenomedullin, Amylin, and Calcitonin Receptors

  title={International Union of Pharmacology. XXXII. The Mammalian Calcitonin Gene-Related Peptides, Adrenomedullin, Amylin, and Calcitonin Receptors},
  author={David R Poyner and Patrick M. Sexton and Ian W. Marshall and David M. Smith and Rémi Quirion and Walter Born and Roman Muff and Jan A. Fischer and Steven M. Foord},
  journal={Pharmacological Reviews},
  pages={233 - 246}
The calcitonin family of peptides comprises calcitonin, amylin, two calcitonin gene-related peptides (CGRPs), and adrenomedullin. The first calcitonin receptor was cloned in 1991. Its pharmacology is complicated by the existence of several splice variants. The receptors for the other members the family are made up of subunits. The calcitonin-like receptor (CL receptor) requires a single transmembrane domain protein, termed receptor activity modifying protein, RAMP1, to function as a CGRP… 

Figures and Tables from this paper

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

This receptor family comprises a group of receptors for the calcitonin/CGRP family of peptides, showing selectivity for CGRP receptors, with a particular preference for those of primate origin.

Intermedin Is a Calcitonin/Calcitonin Gene-related Peptide Family Peptide Acting through the Calcitonin Receptor-like Receptor/Receptor Activity-modifying Protein Receptor Complexes*

In vivo studies demonstrated that intermedin treatment led to blood pressure reduction in both normal and spontaneously hypertensive rats via interactions with the CRLR/RAMP receptor complexes and will allow development of new therapeutic agents for pathologies associated with diverse vascular and gastrointestinal disorders.

Calcitonin receptors in GtoPdb v.2021.2

This receptor family comprises a group of receptors for the calcitonin/CGRP family of peptides and there are several approved drugs that target this receptor family, such as pramlintide, erenumab, and the "gepant" class of CGRP receptor antagonists.

Vascular actions of calcitonin gene-related peptide and adrenomedullin.

The receptor-mediated vascular activities of calcitonin gene-related peptide (CGRP) and the structurally related peptide adrenomedullin are summarized, and potential therapeutic applications based on use of antagonists and gene targeting of agonists are discussed.

Calcitonin Receptor Agents

Pharmacological and Kinetic Characterization of Adrenomedullin 1 and Calcitonin Gene-Related Peptide 1 Receptor Reporter Cell Lines

A novel, aequorin luminescence-based G protein-coupled receptor reporter assay that enables the real-time detection of receptor activation in living cells and established and characterized stable ADM1 and CGRP1 receptor cell lines.

Receptor Activity-modifying Protein-directed G Protein Signaling Specificity for the Calcitonin Gene-related Peptide Family of Receptors*

It is shown that the CGRP family of receptors displays both ligand- and RAMP-dependent signaling bias among the Gαs, Gαi, and Gαq/11 pathways.

Adrenomedullin and calcitonin gene-related peptide receptors in endocrine-related cancers: opportunities and challenges.

To effectively distinguish AM1 and AM2 receptors, selective receptor antagonists need to be developed, and the development of specific CGRP receptor antagonists suggests that this is now feasible.

Pharmacological Discrimination of Calcitonin Receptor: Receptor Activity-Modifying Protein Complexes

The data indicate that careful use of combinations of agonists and antagonists may allow pharmacological discrimination of CT(a, AMY1(a), and AMY3(a) receptors, providing a means to delineate the physiological significance of these receptors.



A cDNA Encoding the Calcitonin Gene-related Peptide Type 1 Receptor (*)

The cloning of a complementary DNA (cDNA) encoding a human CGRP receptor, which shares significant peptide sequence homology with the human calcitonin receptor, a member of the G-protein-coupled receptor superfamily, is reported here.

Multiple ramp domains are required for generation of amylin receptor phenotype from the calcitonin receptor gene product.

Calcitonin (CT), calcitonin gene-related peptide (CGRP), amylin, and adrenomedullin constitute a family of structurally related peptides that signal via either the calcitonin receptor-like receptor

Multiple amylin receptors arise from receptor activity-modifying protein interaction with the calcitonin receptor gene product.

The data suggest that in the CT family of receptors, and potentially in other class II G protein-coupled receptors, the cellular phenotype is likely to be dynamic in regard to the level and combination of both the receptor and the RAMP proteins.

Limitations in using peptide drugs to characterize calcitonin gene-related peptide receptors.

The aim was to identify factors that may limit the use of these drugs to characterize CGRP receptor subtypes and found that maximal relaxation of coronary arteries caused by Cys(Acm)2,7-h-alphaCGRP was dependent upon the level of contractile tone induced by KCl.

A receptor activity modifying protein (RAMP)2-dependent adrenomedullin receptor is a calcitonin gene-related peptide receptor when coexpressed with human RAMP1.

Recognition of RAMP1 and -2 as mediators of CRLR expression as a CGRP or ADM receptor has been extended, with evidence that endogenous RAMP2 is sufficient to reveal an ADM receptors in UMR-106 cells.

Functional Expression of Heteromeric Calcitonin Gene-related Peptide and Adrenomedullin Receptors in Yeast*

The first functional reconstitution of a heteromeric seven transmembrane receptor in yeast suggests this organism as a useful research tool to study the molecular nature of other heteromers, including calcitonin receptor-like receptors.

Identification of an orphan receptor gene as a type 1 calcitonin gene-related peptide receptor.

  • S. KapasA. Clark
  • Biology, Chemistry
    Biochemical and biophysical research communications
  • 1995
The RDC-1 gene was expressed in COS-7 cells and showed a dose dependant increase of cAMP in response to CGRP and adrenomedullin but there was no cAMP response to amylin or [Cys(acm)2,7]a-hCGRP.

Characterization of receptors for calcitonin gene‐related peptide and adrenomedullin on the guinea‐pig vas deferens

This affinity was unaltered by increasing the temperature from 4°C to 25°C, suggesting the anomalous behaviour of CGRP8–37 is not due to temperature differences between binding and functional assays, and this antagonist displaced [125I]‐CGRP with high affinity from vas deferens membranes.

Adrenomedullin and related peptides: receptors and accessory proteins

Pharmacological characterization of receptor-activity-modifying proteins (RAMPs) and the human calcitonin receptor.