Clinically relevant Ω-loop mutations in PDC-3 reshape active-site dynamics to enhance β-lactamase activity, providing mechanistic insights that can guide the rational design of inhibitors.
Liudmyla Arifova, Brian S MacTavish ... Douglas J Kojetin
Covalent PPARγ inhibitors that better stabilize a repressive conformation are more effective inhibitors, but structural plasticity still allows ligand cobinding by enabling a shift back to an active conformation.
Formation and stability of endocytic receptor-arrestin complexes during clathrin-mediated endocytosis are governed by phosphorylation-dependent arrestin-AP2 interactions.
BK and CaV1.3 channels interact early during biogenesis, assembling intracellularly before membrane localization, indicating coordinated processes for functional coupling.
Modestas Matusevicius, Robin A Corey ... Simone Weyand
Cryo-EM structures of human aquaporin AQP2 bound to the anti-trypanosomal drugs pentamidine and melarsoprol identify the molecular mechanism for drug-resistant sleeping sickness.
