Patrick M Killoran, Vicky Capel, Vera D'Aloisio, Adam Schofield, Tímea Aczél, Kata Bölcskei, Zsuzsanna Helyes, Bengt von Mentzer, David A Kendall, Chris R Coxon, Gillian A Hutcheon
OBJECTIVES: It has previously been shown that the peptide (34Pro,35Phe)CGRP27-37 is a potent calcitonin gene-related peptide, CGRP receptor antagonist, and in this project we aimed to improve the antagonist potency through the structural modification of truncated C-terminal CGRP peptides. METHODS: Six peptide analogues were synthesized and the anti-CGRP activity confirmed using both in vitro and in vivo studies. KEY FINDINGS: A 10 amino acid-containing peptide VPTDVGPFAF-NH2 (P006) was identified as a key candidate to take forward for in vivo evaluation, where it was shown to be an effective antagonist after intraperitoneal injection into mice...
September 23, 2023: Journal of Pharmacy and Pharmacology