Structure of a lasso peptide bound ETB receptor provides insights into the mechanism of GPCR inverse agonism
W. Shihoya, H. Akasaka, P. A. Jordan, A. Lechne, B. K. Okada, G. C. M. d. Cruz, F. K. Sano, T. Tanaka, R. Kawahara, R. Chaudhari, H. Masamune, B. J. Mark, O. Nureki
The paper reports cryo-EM structures of the ETB receptor bound to the lasso peptide RES-701-3, revealing its inverse agonist mechanism through hydrophobic interactions and conformational stabilization.
bioRxiv · Dec 30, 2023Biochemistry