Xuan Hong

TL;DR: Through screening and lead optimization using the human PERK crystal structure, compound 38 (GSK2606414), an orally available, potent, and selective PERK inhibitor is discovered, which inhibits PERK activation in cells and inhibits the growth of a human tumor xenograft in mice.

TL;DR: The discovery of inhibitors that fill this void with an unprecedented metal-binding group, trifluoromethyloxadiazole (TFMO), which circumvents the selectivity and pharmacologic liabilities of hydroxamates is reported.

TL;DR: DPH represents the first cell-permeable, small-molecule tool compound for c-Abl activation and binds to the myristoyl binding site and prevents the formation of the bent conformation of the αI helix through steric hindrance.

TL;DR: A scaffold-hop, which exploited the improved physicochemical properties of a dihydropyrazole analogue, identified through fragment screening, delivered potent, soluble, cell-active c-Abl activators, which demonstrated the intracellular activation of c- abl in vivo.

TL;DR: A high-throughput fluorescence polarization assay was developed, which allows detection of Lys-1201 sumoylation, corresponding to the major site of functional sumoylated within the transcriptional repressor trichorhino-phalangeal syndrome type I protein (TRPS1).