Calcitonin Gene Related Peptide Receptor
| Calcitonin Gene Related Peptide Receptor | ||
|---|---|---|
| Properties of human protein | ||
| Mass / length primary structure | 439 amino acids | |
| Secondary to quaternary structure | Heterodimer | |
| Cofactor | RAMP1 / 2/3 | |
| Identifier | ||
| Gene name | CALCRL | |
| External IDs | ||
| Occurrence | ||
| Parent taxon | Vertebrates | |
The calcrl (short CGRP receptor , CGRPR ) is in the cell membrane of vertebrate animals occurring protein obtained by the calcitonin gene-related peptide is activated (CGRP). It is a G protein-coupled receptor that mediates its effects via activation of G s proteins and subsequent activation of adenylyl cyclases . The calcitonin gene-related peptide receptor is identical in its amino acid sequence to the calcitonin receptor-like receptor(CLR) and the adrenomedullin receptor . Its function as a receptor for the calcitonin gene-related peptide is determined by the binding of the receptor activity-modifying protein RAMP1. The calcitonin gene-related peptide receptor plays an important role in the development of a migraine attack . Calcitonin gene-related peptide receptor antagonists , such as olcegepant and telcacepant , have been shown to be effective against migraine in clinical studies and are considered to be potential new therapeutic agents for migraine.
biochemistry
Due to its biochemical properties, the calcitonin gene-related peptide receptor is a popular research object. The receptor is encoded by the gene for the calcitonin receptor-like receptor, which is located on chromosome 2 in the q31-q32 gene locus . Once expressed, the calcitonin receptor-like receptor interacts with receptor activity-modifying proteins to form dimers or higher oligomers. Depending on the bound receptor activity-modifying protein, the calcitonin receptor-like receptor behaves as a calcitonin gene-related peptide receptor or as an adrenomedullin receptor. If the calcitonin receptor-like receptor is present as a dimer with RAMP1, it functions as a calcitonin gene-related peptide receptor.
Individual evidence
- ↑ Homologues at OMA
- ↑ a b Conner AC, Simms J, Barwell J, Wheatley M, Poyner DR: Ligand binding and activation of the CGRP receptor . In: Biochem. Soc. Trans. . 35, No. Pt 4, August 2007, pp. 729-32. doi : 10.1042 / BST0350729 . PMID 17635135 .