Yen Ting Chen

TL;DR: The effect of the vinyl sulfone cysteine proteinase inhibitors K11777 and WRR483 on invasion of human colonic xenografts strongly suggests a significant role of secreted amebic proteinases, such as EhCP1, in the pathogenesis of amebiasis.

TL;DR: The synthesis and optimization of piperidine benzimidazolone MOR agonists that together display a wide range of bias (G/βarr2) are described and structural features affecting potency and maximizing bias are identified and it is shown that many compounds have desirable properties, such as long half-lives and high brain penetration.

TL;DR: Ch chroman-3-amides are reported as highly potent ROCK inhibitors with sufficient kinase selectivity, excellent cell activity, good microsomal stability, and desirable pharmacokinetic properties for study as potential therapeutic agents.

TL;DR: The binding mode of K11002 to cruzain, the major cysteine protease of Trypanosoma cruzi was used in the design of conformationally constrained inhibitors, and Vinyl sulfone-containing macrocycles were synthesized via olefin ring-closing metathesis and evaluated against Cruzain and the closely related cysteined protease, rhodesain.