Beyond structure: emerging approaches to study GPCR dynamics.
By A. Gusach, I. Maslov, A. Luginina, V. Borshchevskiy, A. Mishin, Vadim Cherezov. 2020
51 citations recorded by the source corpus.
G protein-coupled receptors (GPCRs) constitute the largest superfamily of membrane proteins that are involved in regulation of sensory and physiological processes and implicated in many diseases. The last decade revolutionized the GPCR field by unraveling multiple high-resolution structures of many different receptors in complexes with various ligands and signaling partners. A complete understanding of the complex nature of GPCR function is, however, impossible to attain without combining static structural snapshots with information about GPCR dynamics obtained by complementary spectroscopic techniques. As illustrated in this review, structure and dynamics studies are now paving the way for understanding important questions of GPCR biology such as partial and biased agonism, allostery, oligomerization, and other fundamental aspects of GPCR signaling.
Subfields: Molecular Biology, Spectroscopy
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Citations in the corpus
- Sampling alternative conformational states of transporters and receptors with AlphaFold2 (2022, background): “For G- protein-coupled receptors (GPCRs), ligand binding on the extra-cellular side triggers structural rearrangements on the intracellular side that initiate downstream signaling ( Wang et al., 2020 ; Gusach et al., 2020 ).”