Linton Steven D
Idun Pharmaceuticals, 9380 Judicial Drive, San Diego, CA 92121, USA.
Curr Top Med Chem. 2005;5(16):1697-717. doi: 10.2174/156802605775009720.
Caspase inhibition has been demonstrated to be therapeutically effective in moderating excessive programmed cell death, or apoptosis. Publications detailing programs in the pharmaceutical industry have been more frequent in recent years, ranging from SAR studies to clinically relevant animal models of disease. A summary of the work published in this exciting new area is presented, outlining the broad applicability of this fundamental cellular mechanism across several disease indications. This area of research has matured to the level of advancing compounds into clinical trials: VX-740 (Pralnacasan) and VX-765 as anti-inflammatory agents, and IDN-6556, a pan-caspase inhibitor as an anti-apoptotic agent.
半胱天冬酶抑制已被证明在调节过度的程序性细胞死亡或凋亡方面具有治疗效果。近年来，制药行业中详细介绍相关项目的出版物越来越频繁，涵盖从构效关系研究到具有临床相关性的疾病动物模型。本文总结了在这个令人兴奋的新领域发表的研究工作，概述了这一基本细胞机制在多种疾病适应症中的广泛适用性。该研究领域已发展到将化合物推进到临床试验阶段：作为抗炎剂的VX-740（普拉那卡森）和VX-765，以及作为抗凋亡剂的泛半胱天冬酶抑制剂IDN-6556。
