Calcitonin gene-related peptide type 1 receptor

UniProt Q16602 Organism Homo sapiens Gene CALCRL, CGRPR

Also known as: CALCRL, CGRPR

Function

G protein-coupled receptor which specificity is determined by its interaction with receptor-activity-modifying proteins (RAMPs). Together with RAMP1, form the receptor complex for calcitonin-gene-related peptides CALCA/CGRP1 and CALCB/CGRP2. Together with RAMP2 or RAMP3, function as receptor complexes for adrenomedullin (ADM and ADM2). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors. Activates cAMP-dependent pathway.

Classification

Family (Pfam): PF00002 7tm_2, PF02793 HRM
InterPro: GPCR_2, GPCR_2-like_7TM, GPCR_2_calcitonin_rcpt_fam, GPCR_2_CGRP1_rcpt, GPCR_2_extracell_dom_sf, GPCR_2_extracellular_dom, GPCR_2_secretin-like, GPCR_2_secretin-like_CS
Functional cluster: G Protein-Coupled Receptors

Experimental structures · PDB · 24

3AQF X-ray 2.60A
3N7P X-ray 2.80A
3N7R X-ray 2.90A
3N7S X-ray 2.10A
4RWF X-ray 1.76A
4RWG X-ray 2.44A
5V6Y X-ray 2.80A
6D1U X-ray 2.05A
6E3Y EM 3.30A
6UMG X-ray 2.70A
6UUN EM 3.00A
6UUS EM 2.40A
… and 12 more

A predicted model is available from AlphaFold.

Gene Ontology · 22

Disease associations

lymphatic malformation 8 MONDO:0032907

Drugs targeting this protein · 11

MK3207 antagonist
OLCEGEPANT antagonist
DAVALINTIDE agonist
RIMEGEPANT antagonist
RIMEGEPANT SULFATE antagonist
UBROGEPANT antagonist
TELCAGEPANT antagonist
ZAVEGEPANT antagonist
BI-44370 antagonist
ATOGEPANT antagonist
ZAVEGEPANT HYDROCHLORIDE antagonist

Related proteins · sequence + function similarity

Co-cited proteins · studied together in the literature

Receptor activity-modifying protein 2 4 shared papers
Receptor activity-modifying protein 1 3 shared papers
Calcitonin gene-related peptide 1 2 shared papers
Receptor activity-modifying protein 3 2 shared papers
Pro-adrenomedullin 2 shared papers
Protein ADM2 1 shared papers
Calcitonin gene-related peptide 2 1 shared papers

Literature · 11 cited papers

Structure and dynamics of the CGRP receptor in apo and peptide-bound forms. Science · 2021
Structure and Dynamics of Adrenomedullin Receptors AM1 and AM2 Reveal Key Mechanisms in the Control of Receptor Phenotype by Receptor Activity-Modifying Proteins. ACS Pharmacol. Transl. Sci. · 2020
hCALCRL mutation causes autosomal recessive nonimmune hydrops fetalis with lymphatic dysplasia. J. Exp. Med. · 2018
Structural basis for extracellular interactions between calcitonin receptor-like receptor and receptor activity-modifying protein 2 for adrenomedullin-specific binding. Protein Sci. · 2012
Crystal structure of the ectodomain complex of the CGRP receptor, a class-B GPCR, reveals the site of drug antagonism. Structure · 2010
Generation and annotation of the DNA sequences of human chromosomes 2 and 4. Nature · 2005
Signal peptide prediction based on analysis of experimentally verified cleavage sites. Protein Sci. · 2004
Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat. Genet. · 2004
RAMPs regulate the transport and ligand specificity of the calcitonin-receptor-like receptor. Nature · 1998
A cDNA encoding the calcitonin gene-related peptide type 1 receptor. J. Biol. Chem. · 1996
A human orphan calcitonin receptor-like structure. Biochem. Biophys. Res. Commun. · 1995

A document in the lmmol reference corpus — open public data (UniProt, GO, PDB, the literature graph) rendered as a single cross-linked page. Hover any link to preview its target.