Publications by authors named "Youngchai Son"
Article Synopsis
- Ubiquitination modifies proteins with ubiquitin to regulate their degradation or functions, while deubiquitinating enzymes (DUBs) remove ubiquitin, influencing these processes.
- USP2a, a DUB, is highlighted as a promising cancer therapy target, but effective inhibitors have been scarce.
- The study focused on optimizing a USP2a inhibitor, ML364, resulting in compound 8v, which showed lower toxicity, reduced USP2a targets, decreased cancer cell growth, and selective inhibition of USP2a compared to other related proteins.
Disruption of protein-protein interaction between transcriptional enhancer factor (TEA)-domain (TEAD; a transcription factor) and its co-activator Yes-associated protein (YAP)/ transcriptional co-activator with PDZ-binding motif (TAZ) is a potential therapeutic strategy against various types of solid tumors. Based on hit compound 8 and 9a, hydrazone derivatives with dioxo-benzo[d]isothiazole (9b-n) and oxime ester (10a-s) or amide derivatives (11a-r) with dioxo-benzo[b]thiophene were designed and synthesized as novel TEAD-YAP interaction inhibitors. Amide derivative 11q exhibited a higher potency in inhibiting TEAD-YAP reporter expression activity (IC = 12.
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