GPCR modulation by RAMPs

Pharmacol Ther. 2006 Jan;109(1-2):173-97. doi: 10.1016/j.pharmthera.2005.06.015. Epub 2005 Aug 18.

Abstract

Our conceptual understanding of the molecular architecture of G-protein coupled receptors (GPCRs) has transformed over the last decade. Once considered as largely independent functional units (aside from their interaction with the G-protein itself), it is now clear that a single GPCR is but part of a multifaceted signaling complex, each component providing an additional layer of sophistication. Receptor activity-modifying proteins (RAMPs) provide a notable example of proteins that interact with GPCRs to modify their function. They act as pharmacological switches, modifying GPCR pharmacology for a particular subset of receptors. However, there is accumulating evidence that these ubiquitous proteins have a broader role, regulating signaling and receptor trafficking. This article aims to provide the reader with a comprehensive appraisal of RAMP literature and perhaps some insight into the impact that their discovery has had on those who study GPCRs.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Humans
  • Intracellular Signaling Peptides and Proteins / genetics
  • Intracellular Signaling Peptides and Proteins / metabolism
  • Intracellular Signaling Peptides and Proteins / pharmacology*
  • Membrane Proteins / genetics
  • Membrane Proteins / metabolism
  • Membrane Proteins / pharmacology*
  • Proteins / pharmacology*
  • Receptor Activity-Modifying Proteins
  • Receptors, G-Protein-Coupled / drug effects*
  • Signal Transduction / drug effects
  • Signal Transduction / physiology

Substances

  • Intracellular Signaling Peptides and Proteins
  • Membrane Proteins
  • Proteins
  • Receptor Activity-Modifying Proteins
  • Receptors, G-Protein-Coupled