Mechanism-based inhibitors of serine proteases with high selectivity through optimization of S’ subsite binding

A series of mechanism-based inhibitors designed to interact with the S’ subsites of serine proteases was synthesized and their inhibitory activity toward the closely-related serine proteases human neutrophil elastase (HNE) and proteinase 3 (PR 3) was investigated. The compounds were found to be time-dependent inhibitors of HNE and were devoid of any inhibitory activity toward PR 3.


Yi Li, Dengfeng Dou, Guijia He, Gerald H. Lushington, William C. Groutas
May 15, 2009
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