Article
Cholesterol-dependent dynamic changes in the conformation of the type 1 cholecystokinin receptor affect ligand binding and G protein coupling.
PLoS biology - 1 Jul 2024
Harikumar Kaleeckal G, Zhao Peishen, Cary Brian P, Xu Xiaomeng, Desai Aditya J, Dong Maoqing, Mobbs Jesse I, Toufaily Chirine, Furness Sebastian G B, Christopoulos Arthur, Belousoff Matthew J, Wootten Denise, Sexton Patrick M, Miller Laurence J
Abstract excerpt
Development of optimal therapeutics for disease states that can be associated with increased membrane cholesterol requires better molecular understanding of lipid modulation of the drug target. Type 1 cholecystokinin receptor (CCK1R) agonist actions are affected by increased membrane cholesterol, enhancing ligand binding and reducing calcium signaling, while agonist actions of the closely related CCK2R are not....
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