Interaction of calcitonin-gene-related peptide with its receptors |
| |
Authors: | Conner A C Hay D L Howitt S G Kilk K Langel U Wheatley M Smith D M Poyner D R |
| |
Affiliation: | Pharmaceutical Sciences Research Institute, Aston University, Birmingham B4 7ET, UK. |
| |
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. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|