Interactions of cholesterol molecules with GPCRs in different states: A comparative analysis of GPCRs' structures

Highlights

• The positions of cholesterol molecules in structures of 68 GPCRs in different states are gathered in an interactive table

• A comparative analysis of CLR number and position is performed between different states of GPCR

• Cholesterol molecules bind differently when some GPCRs adopt a ligand-bound state

• The type of ligands and intracellular binders affect the interaction of CLR in several GPCR structures

Abstract

GPCRs form a very large family of transmembrane proteins involved in a wide range of physiological functions. Some GPCRs have their activity affected by the presence of cholesterol either indirectly through changes in the physical properties of the membrane or directly by binding to the receptor. Thanks to recent advances in structural biology, many structures of GPCRs have been solved, 240 of which contain at least one cholesterol molecule or surrogate. This review lists the position of these molecules and provides a comparative analysis of the changes observed in the structures depending on the state of the receptor.