Calcitonin Gene-Related Peptides (CGRP) and Fragments

Introduction

Calcitonin gene-related peptide (CGRP) is the first neuropeptide that is genetically recombined and biosynthesized. CGRP is a well-characterized peptide consisting of 37 amino acids. There are two subtypes of α and β, which are encoded by the α-CGRP gene and the β-CGRP gene, respectively. It is distributed in the central and peripheral tissues. α-CGRP is widely expressed in the central and peripheral nervous systems. The expression of β-CGRP is relatively restricted, but it is also present throughout the central nervous system, vasculature, and enteric nerves.

Mechanism of action

CGRP is a major neurotransmitter of capsaicin-sensitive sensory nerves, which is synthesized in neuronal bodies and stored in nerve endings. The synthesis and release of CGRP is regulated by a variety of factors. The transient receptor potential channel vanilloid type 1 (TRPV1) is a key receptor regulating the synthesis and release of CGRP. TRPV1 binding site is located inside the cell membrane. TRPV1's endogenous ligand, anandamide, is transported into the cell by the transporter to function. CGRP interacts with CGRP receptors to exert an effect.

Application of CGRP

CGRP has a wide and complex biological effect. In nerve tissue, CGRP is associated with neuralgia and migraine attacks. In the cardiovascular system, in addition to regulating vascular tone and maintaining circulatory stability, CGRP can also reduce ischemic injury, inhibit myocardial fibroblast proliferation and cardiac remodeling. In the gastrointestinal tract, CGRP has a protective effect on the gastric mucosa. CGRP is involved in the pathophysiological processes of various cardiovascular diseases such as hypertension, myocardial infarction, heart failure and pulmonary hypertension. Exogenous CGRP can be used to treat hypertension, pulmonary hypertension, acute lung injury, brain and heart ischemia-reperfusion injury, and chronic heart failure. Therefore, it is speculated that affecting the synthesis and release of endogenous CGRP may be a new way to find new drugs.

Reference

1. Chai, W., Mehrotra, S., Jan Danser, A.H., Schoemaker, R.G. (2006) The role of calcitonin gene- related peptide (CGRP) in ischemic preconditioning in isolated rat hearts. Eur J Pharmacol, 531: 246-253.