Structure-based Evolution of G protein-biased μ-opioid Receptor Agonists
H. Wang, F. Hetzer, W. Huang, Q. Qu, J. Meyerowitz, J. Kaindl, H. Huebner, G. Skiniotis, B. Kobilka, P. Gmeiner
The paper reports cryoEM structures of the μ-opioid receptor bound to biased agonists PZM21 and FH210, revealing structural basis for reduced β-arrestin recruitment and guiding development of safer analgesics.
bioRxiv · Mar 22, 2022Pharmacology & Toxicology