期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 48, 期 22, 页码 6779-6782出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm050307e
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A series of oxamyl dipeptides were optimized for pan caspase inhibition, anti-apoptotic cellular activity and in vivo efficacy. This structure-activity relationship study focused on the P4 oxamides and warhead moieties. Primarily on the basis of in vitro data, inhibitors were selected for study in a murine model of alpha-Fas-induced liver injury. IDN-6556 (1) was further profiled in additional in vivo models and pharmacokinetic studies. This first-in-class caspase inhibitor is now the subject of two Phase 11 clinical trials, evaluating its safety and efficacy for use in liver disease.
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