Biased activation of the vasopressin V2 receptor probed by NMR, paramagnetic ligands, and molecular dynamics simulations
G. Gaibelet, A. Fouillen, R. Stephanie, H. Orcel, C. Mendre, A. Kanso, R. Lanotte, J. Nguyen, J. Dimon, S. Urbach, R. Sounier, S. Granier, D. Bonnet, X. Cong, B. Mouillac, H. Demene
The paper uses NMR, molecular dynamics, and pharmacology to study conformational changes in the V2R receptor bound to different ligands, revealing a mechanism for Gs-biased agonism involving TM7 and TM3 interactions.
bioRxiv · Jun 6, 2023 · PreprintBiophysics