Article
Dynamics of GLP-1R peptide agonist engagement are correlated with kinetics of G protein activation.
Nature communications - 10 Jan 2022
Deganutti Giuseppe, Liang Yi-Lynn, Zhang Xin, Khoshouei Maryam, Clydesdale Lachlan, Belousoff Matthew J, Venugopal Hari, Truong Tin T, Glukhova Alisa, Keller Andrew N, Gregory Karen J, Leach Katie, Christopoulos Arthur, Danev Radostin, Reynolds Christopher A, Zhao Peishen, Sexton Patrick M, Wootten Denise
Abstract excerpt
The glucagon-like peptide-1 receptor (GLP-1R) has broad physiological roles and is a validated target for treatment of metabolic disorders. Despite recent advances in GLP-1R structure elucidation, detailed mechanistic understanding of how different peptides generate profound differences in G protein-mediated signalling is still lacking. Here we combine cryo-electron microscopy, molecular dynamics simulations,...
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