CHISHIKI

Drug Discovery

Recent Developments in Therapeutic Peptides for the Glucagon-like Peptide 1 and 2 Receptors

By Rie Suzuki, Giles Brown, John Christopher, Conor Scully and Miles Congreve | Oct 4, 2019

Summary  

Dr. Rie Suzuki, Director, Translational Sciences at Sosei Heptares, recently published a Review article titled “Recent Developments in Therapeutic Peptides for the Glucagon-like Peptide 1 and 2 Receptors” in the Journal of Medicinal Chemistry, alongside Giles Brown from OMass Therapeutics and fellow Sosei Heptares colleagues John Christopher, Conor Scully and Miles Congreve.

 

Abstract

Glucagon-like peptide-1 (GLP-1) and glucagon-like peptide-2 (GLP-2) are proglucagon derived peptides that are released from gut endocrine cells in response to nutrient intake. These molecules are rapidly inactivated by the action of dipeptidyl peptidase IV which limit their use as therapeutic agents. The recent emergence of three-dimensional structures of GPCRs such as GLP-1R and glucagon receptor has helped to drive the rational design of innovative peptide molecules that hold promise as novel peptide therapeutics. One emerging area is the discovery of multifunctional molecules that act at two or more pharmacological systems to enhance therapeutic efficacy.  In addition, drug discovery efforts are also focusing on strategies to improve patient convenience through alternative routes of peptide delivery. These novel strategies highlight the broad utility of peptide-based therapeutics in human disease settings where unmet needs still exist.

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