Comparing the molecular pharmacology of CGRP and adrenomedullin
- PMID: 23745700
- DOI: 10.2174/13892037113149990053
Comparing the molecular pharmacology of CGRP and adrenomedullin
Abstract
CGRP and adrenomedullin [AM] are peptides that have a number of physiological effects, including vasodilation, through the activation of a shared GPCR, the family B calcitonin receptor-like receptor [CLR]. Specificity to each ligand is conferred through the unusual association of CLR with a single transmembrane accessory protein. For CGRP this is receptor activity-modifying protein 1 [RAMP1] and for AM acting at the AM1 receptor this is RAMP2. Receptor signalling by two specific peptide ligands through a common GPCR provides researchers with vital and unique information into similarities and differences of GPCR activation. Understanding the structure and function of these receptors will also provide a platform for future drug design for a number of cardiovascular and metabolic diseases in which CGRP and AM have been implicated. This review summarises the latest information and data concerning ligand binding, receptor activation and structural studies for both the CGRP and AM receptors.
Similar articles
-
Structure-function analyses reveal a triple β-turn receptor-bound conformation of adrenomedullin 2/intermedin and enable peptide antagonist design.J Biol Chem. 2018 Oct 12;293(41):15840-15854. doi: 10.1074/jbc.RA118.005062. Epub 2018 Aug 23. J Biol Chem. 2018. PMID: 30139742 Free PMC article.
-
Probing the Mechanism of Receptor Activity-Modifying Protein Modulation of GPCR Ligand Selectivity through Rational Design of Potent Adrenomedullin and Calcitonin Gene-Related Peptide Antagonists.Mol Pharmacol. 2018 Apr;93(4):355-367. doi: 10.1124/mol.117.110916. Epub 2018 Jan 23. Mol Pharmacol. 2018. PMID: 29363552 Free PMC article.
-
Receptor activity-modifying protein-dependent effects of mutations in the calcitonin receptor-like receptor: implications for adrenomedullin and calcitonin gene-related peptide pharmacology.Br J Pharmacol. 2014 Feb;171(3):772-88. doi: 10.1111/bph.12508. Br J Pharmacol. 2014. PMID: 24199627 Free PMC article.
-
Protective effects of intermedin on cardiovascular, pulmonary and renal diseases: comparison with adrenomedullin and CGRP.Curr Protein Pept Sci. 2013 Jun;14(4):294-329. doi: 10.2174/13892037113149990049. Curr Protein Pept Sci. 2013. PMID: 23745696 Review.
-
The pharmacology of adrenomedullin receptors and their relationship to CGRP receptors.J Mol Neurosci. 2004;22(1-2):105-13. doi: 10.1385/JMN:22:1-2:105. J Mol Neurosci. 2004. PMID: 14742915 Review.
Cited by
-
Calcitonin Gene-Related Peptide Regulates Cardiomyocyte Survival through Regulation of Oxidative Stress by PI3K/Akt and MAPK Signaling Pathways.Ann Clin Exp Hypertens. 2014 Jan;2(1):1007. Ann Clin Exp Hypertens. 2014. PMID: 25478604 Free PMC article.
-
Receptor Activity-modifying Protein-directed G Protein Signaling Specificity for the Calcitonin Gene-related Peptide Family of Receptors.J Biol Chem. 2016 Oct 14;291(42):21925-21944. doi: 10.1074/jbc.M116.751362. Epub 2016 Aug 26. J Biol Chem. 2016. PMID: 27566546 Free PMC article.
-
Ocular redness - II: Progress in development of therapeutics for the management of conjunctival hyperemia.Ocul Surf. 2021 Jul;21:66-77. doi: 10.1016/j.jtos.2021.05.004. Epub 2021 May 15. Ocul Surf. 2021. PMID: 34000363 Free PMC article. Review.
-
hCALCRL mutation causes autosomal recessive nonimmune hydrops fetalis with lymphatic dysplasia.J Exp Med. 2018 Sep 3;215(9):2339-2353. doi: 10.1084/jem.20180528. Epub 2018 Aug 16. J Exp Med. 2018. PMID: 30115739 Free PMC article.
-
The Importance of Understanding Amylin Signaling Mechanisms for Therapeutic Development in the Treatment of Alzheimer's Disease.Curr Pharm Des. 2020;26(12):1345-1355. doi: 10.2174/1381612826666200318151146. Curr Pharm Des. 2020. PMID: 32188374 Free PMC article. Review.
Publication types
MeSH terms
Substances
Grants and funding
LinkOut - more resources
Full Text Sources
Other Literature Sources
Research Materials