Submitted by D.P. Juan on Wed, 13/12/2023 - 14:37
The Mela Group recently published a paper on "Molecular Mechanisms of Cationic Fusogenic Liposome Interactions with Bacterial Envelopes" in the Journal of the American Chemical Society. This paper looked at the interactions between liposomes, bacteria and how they merged together.
Read the paper here: https://pubs.acs.org/doi/10.1021/jacs.3c11463
The Miller Group has published its work on GABA-A receptor α5 selective modulators, in Nature Structural and Molecular Biology. Read the paper here: https://www.nature.com/articles/s41594-023-01133-1.
They engineered an α5 X-ray/Cryo-EM structure platform which retained native binding modes for drugs at the “benzodiazepine” site. They selected α5 for its selective pharmacology and relevance to learning disorders such as cognitive impairment associated with schizophrenia.
They used radioligand binding, ePhys and cryo-EM studies to give detailed insight into b-carboline, benzo, and isoxazole selectivity. The group gives special thanks to Maria-Clemencia Hernandez & Giuseppe Cecere at Roche for support and for the compounds they provided.
For the isoxazoles they observed interesting pocket displacements between negative vs positive modulators, the first such structure-activity relationship observed for a GABA-A receptor. Their hope is that this study can empower future drug-design efforts against this valuable target.
