Modulating receptor function through RAMPs: can they represent drug targets in themselves?

Patrick M Sexton, David R Poyner, John Simms, Arthur Christopoulos, Debbie L Hay

Research output: Contribution to journalReview article

53 Citations (Scopus)

Abstract

G protein-coupled receptors (GPCRs) are successfully exploited as drug targets. As our understanding of how distinct GPCR subtypes can be generated expands, so do possibilities for therapeutic intervention via these receptors. Receptor activity-modifying proteins (RAMPs) are excellent examples of proteins that enhance diversity in GPCR function. They facilitate the creation of binding pockets, controlling the pharmacology of some GPCRs. Moreover, they have the ability to regulate cell-surface trafficking, internalisation and signalling of GPCRs, creating novel opportunities for drug discovery. RAMPs could be directly targeted by drugs, or advantage could be taken of unique RAMP/GPCR interfaces for generating highly selective ligands.

Original languageEnglish
Pages (from-to)413-419
Number of pages7
JournalDrug Discovery Today
Volume14
Issue number7-8
DOIs
Publication statusPublished - Apr 2009

Keywords

  • Animals
  • Binding Sites
  • Drug Delivery Systems
  • Drug Design
  • Humans
  • Intracellular Signaling Peptides and Proteins
  • Membrane Proteins
  • Molecular Structure
  • Protein Binding
  • Protein Transport
  • Receptor Activity-Modifying Proteins
  • Receptors, G-Protein-Coupled
  • Signal Transduction
  • Journal Article
  • Review

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