CGRP and Migraine: The Role of Blocking Calcitonin Gene-Related Peptide Ligand and Receptor in the Management of Migraine

Drugs ◽  
2018 ◽  
Vol 78 (9) ◽  
pp. 913-928 ◽  
Author(s):  
Kasra Maasumi ◽  
Rebecca L. Michael ◽  
Alan M. Rapoport
Keyword(s):  
Calcitonin Gene Related Peptide ◽  
Peptide Ligand ◽  
Related Peptide ◽  
Calcitonin Gene

Role of calcitonin gene-related peptide in energy metabolism

Endocrine ◽  
2017 ◽  
Vol 58 (1) ◽  
pp. 3-13 ◽  
Author(s):  
William Gustavo Lima ◽  
Gleuber Henrique Marques-Oliveira ◽  
Thaís Marques da Silva ◽  
Valéria Ernestânia Chaves
Keyword(s):  
Energy Metabolism ◽  
Calcitonin Gene Related Peptide ◽  
Related Peptide ◽  
Calcitonin Gene

scholarly journals Role of calcitonin gene-related peptide in gastric hypersensitivity in rats

2006 ◽  
Vol 14 (25) ◽  
pp. 2484
Author(s):  
Fei-Fei Zhang ◽  
Jian-Zhong Mo ◽  
You-Ling Lv ◽  
Sheng-Liang Chen ◽  
Ming Lv ◽  
...  
Keyword(s):  
Calcitonin Gene Related Peptide ◽  
Related Peptide ◽  
Calcitonin Gene

scholarly journals Exploring Ligand Binding to Calcitonin Gene-Related Peptide Receptors

2021 ◽  
Vol 8 ◽  
Author(s):  
Giuseppe Deganutti ◽  
Silvia Atanasio ◽  
Roxana-Maria Rujan ◽  
Patrick M. Sexton ◽  
Denise Wootten ◽  
...  
Keyword(s):  
Molecular Dynamics ◽  
Ligand Binding ◽  
Calcitonin Gene Related Peptide ◽  
Related Peptide ◽  
Calcitonin Gene ◽  
Approved Drugs ◽  
G Protein Coupled ◽  
Dynamic Docking ◽  
Receptor Family

Class B1 G protein-coupled receptors (GPCRs) are important targets for many diseases, including cancer, diabetes, and heart disease. All the approved drugs for this receptor family are peptides that mimic the endogenous activating hormones. An understanding of how agonists bind and activate class B1 GPCRs is fundamental for the development of therapeutic small molecules. We combined supervised molecular dynamics (SuMD) and classic molecular dynamics (cMD) simulations to study the binding of the calcitonin gene-related peptide (CGRP) to the CGRP receptor (CGRPR). We also evaluated the association and dissociation of the antagonist telcagepant from the extracellular domain (ECD) of CGRPR and the water network perturbation upon binding. This study, which represents the first example of dynamic docking of a class B1 GPCR peptide, delivers insights on several aspects of ligand binding to CGRPR, expanding understanding of the role of the ECD and the receptor-activity modifying protein 1 (RAMP1) on agonist selectivity.

Protective role of calcitonin gene-related peptide on acute and chronic gut inflammation in rats

1998 ◽  
Vol 114 ◽  
pp. A1035
Author(s):  
L. Mazelin ◽  
V. Theodorou ◽  
J. Fioramonti ◽  
L. Bueno
Keyword(s):  
Calcitonin Gene Related Peptide ◽  
Protective Role ◽  
Gut Inflammation ◽  
Related Peptide ◽  
Calcitonin Gene

Effects of calcitonin gene-related peptide on vascular resistance in rats: role of sex steroids

1999 ◽  
Vol 276 (6) ◽  
pp. H2063-H2068 ◽  
Author(s):  
Michelle Grewal ◽  
Janis Cuevas ◽  
Gautam Chaudhuri ◽  
Lauren Nathan
Keyword(s):  
Sex Steroids ◽  
Perfusion Pressure ◽  
Pressor Response ◽  
Calcitonin Gene Related Peptide ◽  
Ovariectomized Rats ◽  
Synthesis Inhibitor ◽  
Pregnant Rats ◽  
Related Peptide ◽  
Calcitonin Gene

It has been demonstrated in reflex-intact animals that the sensitivity to calcitonin gene-related peptide (CGRP) is increased during pregnancy and that this action is mediated by sex steroids but not by nitric oxide (NO). We assessed the effects of CGRP in the following groups of anesthetized ganglion-blocked rats: 1) pregnant, 2) ovariectomized, and 3) ovariectomized and treated with estradiol and progesterone. Changes in mean arterial pressure (MAP) were assessed after the administration of varying doses of CGRP. Decreases in MAP after CGRP administration were significantly greater in pregnant rats and ovariectomized rats administered sex steroids than in ovariectomized controls. The CGRP antagonist CGRP8–37 produced a pressor response of similar magnitude in both pregnant and ovariectomized rats. We also assessed the effects of CGRP and the modulating role of NO in the isolated uterine vascular bed preparation. CGRP reduced perfusion pressure to a greater degree in ovariectomized animals treated with sex steroids than in ovariectomized animals. This response was attenuated by pretreatment with an NO synthesis inhibitor. CGRP8–37 produced a similar increase in perfusion pressure in both groups. We conclude that 1) the increased vascular sensitivity observed during pregnancy or after treatment with sex steroids is in part mediated by NO, and 2) CGRP8–37 has a vasoconstrictor action of its own.

Sign in / Sign up

Export Citation Format

Share Document