Energy Landscapes Reveal Agonist Control of G Protein-Coupled Receptor Activation via Microswitches
Oliver Fleetwood, Pierre Matricon, Jens Carlsson, Lucie Delemotte
Abstract
. The agonist binding site hence communicates with the intracellular region via a cascade of locally connected microswitches. Characterization of these can be used to understand how ligands stabilize distinct receptor states and contribute to development drugs with specific signaling properties. The developed simulation protocol can likely be transferred to other class A GPCRs.
Topics & Concepts
AgonistChemistryReceptorBiochemistryReceptor Mechanisms and SignalingSingle-cell and spatial transcriptomicsLipid Membrane Structure and Behavior