Pyridine-based allosteric inhibitors selectively target HIV-1 integrase tetramers and exhibit enhanced antiviral activity against a dolutegravir resistant mutant virus indicating potential clinical benefits for combining these two classes of inhibitors.
Unique methodology was used to generate a large HDX-MS dataset to inform ligand-mediated activation of RORγ, an approach that can be extended to other nuclear receptors with unresolved ligand-dependent activities.
Combination of stem cell engineering and CRISPR technologies created a facile method to genetically manipulate macrophages, a multifunctional cell type that plays critical roles in immunity, cancer, and tissue homeostasis.
A fish-derived bile salt was shown to act as interspecific infochemical, inducing the widespread predator avoidance behavior diel vertical migration at picomolar concentrations in freshwater zooplankton of the genus Daphnia.
A network of the gut chemical landscape predicts microbe-mediated biotransformation of foods and drugs and supports the generation of mechanistic hypotheses of microbiome metabolic phenotypes that shape human biology.
The C2-domain of cytoplasmic phospholipase A2α is structurally designed to target PC-rich membrane regions to increase the enzymatic efficiency of the catalytic domain, which prefers PCs with polyunsaturated acyl chains.