44 2033180199
All submissions of the EM system will be redirected to Online Manuscript Submission System. Authors are requested to submit articles directly to Online Manuscript Submission System of respective journal.
Journal of Pharmacology and Medicinal Chemistry

Sign up for email alert when new content gets added: Sign up

G protein activation's correlation with the dynamics of GLP-1R peptide agonist engagement

Author(s): Nicole Watson

The Glucagon-like Peptide-1 Receptor (GLP-1R) has a wide range of physiological functions and is a well-established therapeutic target for metabolic diseases. Despite recent progress in elucidating the structure of the GLP-1R, a full mechanistic understanding of how various peptides create dramatic variations in G protein-mediated signalling is still absent. To investigate the mechanism and implications of GLP-1R binding to four peptide agonists, we used cryo-electron microscopy, molecular dynamics simulations, receptor mutagenesis, and pharmacological experiments. These findings show that differences in peptide N-terminal contacts and dynamics with the GLP-1R transmembrane domain are linked to variances in G protein allosteric coupling.

Google Scholar citation report
Citations : 18

Journal of Pharmacology and Medicinal Chemistry received 18 citations as per Google Scholar report

Global Tech Summit Top