Kaixian Chen

TL;DR: Although the compounds induced mitochondrial potential reduction, caspase activation, and ROS generation, the cytotoxicities and the ultrastructural changes of outer mitochondrial membrane suggested that the compounds may target additional proteins outside the Bcl-2 family.

TL;DR: DC-TEADin02 was identified as the most potent, selective, covalent TEAD autopalmitoylation inhibitor with the IC50 value of 197 ± 19 nM while it showed minimal effect on TEAD-YAP interaction, and proved the validity of modulating transcriptional output in the Hippo signaling pathway through irreversible chemical interventions of TEADs autopalMIToylation activity.

TL;DR: Four candidate compounds found by virtual screening were investigated by using the whole-cell voltage-clamp recording in rat dissociated hippocampal neurons, and intracellular application of the four compounds had no effect on both the K(+) currents.

TL;DR: Application of D3Pockets on 5 target proteins as examples, namely, HIV-1 protease, BACE1, L-ABP, GPX4 and GR, uncovers more information of the dynamic properties of the ligand-binding pockets, which should be helpful to understanding protein function mechanism and drug design.

TL;DR: This is the first report of a synergistic glucose- and lipid-lowering effect of BVC and synthetic agonists induced by unique binding with PPAR-γ or -α, which may improve the efficacy and decrease the toxicity of marketed drugs for use as adjunctive therapy to treat the metabolic syndrome.