2. Academic Validation
  3. Receptor activity-modifying proteins; multifunctional G protein-coupled receptor accessory proteins

Receptor activity-modifying proteins; multifunctional G protein-coupled receptor accessory proteins

  • Biochem Soc Trans. 2016 Apr 15;44(2):568-73. doi: 10.1042/BST20150237.
Debbie L Hay 1,  Christopher S Walker 2,  Joseph J Gingell 2,  Graham Ladds 3,  Christopher A Reynolds 4,  David R Poyner 5
Affiliations

Affiliations

  • 1 School of Biological Sciences, University of Auckland, Auckland 1010, New Zealand [email protected] [email protected].
  • 2 School of Biological Sciences, University of Auckland, Auckland 1010, New Zealand.
  • 3 Department of Pharmacology, Cambridge University, Cambridge CB2 1PD, U.K.
  • 4 School of Biological Sciences, Essex University, Colchester CO4 3SQ, U.K.
  • 5 School of Life and Health Sciences, Aston University, Birmingham B4 7ET, U.K. [email protected] [email protected].
PMID: 27068971 DOI: 10.1042/BST20150237
Abstract

Receptor activity-modifying proteins (RAMPs) are single pass membrane proteins initially identified by their ability to determine the pharmacology of the Calcitonin receptor-like receptor (CLR), a family B G protein-coupled receptor (GPCR). It is now known that RAMPs can interact with a much wider range of GPCRs. This review considers recent developments on the structure of the complexes formed between the extracellular domains (ECDs) of CLR and RAMP1 or RAMP2 as these provide insights as to how the RAMPs direct ligand binding. The range of RAMP interactions is also considered; RAMPs can interact with numerous family B GPCRs as well as examples of family A and family C GPCRs. They influence receptor expression at the cell surface, trafficking, ligand binding and G protein coupling. The GPCR-RAMP interface offers opportunities for drug targeting, illustrated by examples of drugs developed for migraine.

Keywords

adrenomedullin; amylin; calcitonin gene-related peptide (CGRP); calcitonin receptor; calcitonin receptor-like receptor; family B G protein-coupled receptor; receptor activity-modifying protein (RAMP).

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