Interaction of calcitonin-gene-related peptide with its receptors

A. C. Conner, D. L. Hay, S. G. Howitt, K. Kilk, Ü Langel, M. Wheatley, D. M. Smith, D. R. Poyner

Research output: Contribution to journalArticle

48 Citations (Scopus)

Abstract

The receptor for calcitonin-gene-related peptide (CGRP) is a heterodimer formed by calcitonin-receptor-like receptor (CRLR), a type II (family B) G-protein-coupled receptor, and receptor-activity-modifying protein 1 (RAMP1), a single-membrane-pass protein. It is likely that the first seven or so amino acids of CGRP (which form a disulphide-bonded loop) interact with the transmembrane domain of CRLR to cause receptor activation. The rest of the CGRP molecule falls into three domains. Residues 28-37 and 8-18 are normally required for high-affinity binding, while residues 19-27 form a hinge region. The 28-37 region is almost certainly in direct contact with the receptor; 8-18 may make additional receptor contacts or may stabilize an appropriate conformation of 28-37. It is likely that these regions of CGRP interact both with CRLR and with the extracellular domain of RAMP1.

Original languageEnglish
Pages (from-to)451-455
Number of pages5
JournalBiochemical Society Transactions
Volume30
Issue number4
DOIs
Publication statusPublished - 1 Aug 2002
Externally publishedYes

Keywords

  • Adrenomedullin
  • Calcitonin-receptor-like receptor (CRLR)
  • CGRP
  • Receptor-activity-modifying protein 1 (RAMPI)
  • Structure-activity relationships

ASJC Scopus subject areas

  • Biochemistry

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