天冬氨酰氧基烷酰基酮和天冬氨酰氨氧烷酰基酮对白细胞介素-1β转换酶（ICE 或半胱天冬酶 1）的抑制作用。
Inhibition of interleukin-1beta converting enzyme (ICE or caspase 1) by aspartyl acyloxyalkyl ketones and aspartyl amidooxyalkyl ketones.
机构信息
Pfizer Global Research and Development, Ann Arbor, MI 48105, USA.
出版信息
Bioorg Med Chem Lett. 2010 Sep 1;20(17):5089-94. doi: 10.1016/j.bmcl.2010.07.031. Epub 2010 Jul 11.
PMID:20674352
Abstract
A series of acyloxyalkyl and amidooxyalkyl ketones appended to a carbobenzyloxy aspartic acid core have been prepared. The most potent of these new inhibitors was 4i with a K(i) of 0.5 microM. These two series provide an improved understanding of the binding requirements for the hydrophobic prime side of ICE.
摘要
已制备了一系列连接到碳苄氧羰基天冬氨酸核心的酰氧基烷基和氨氧基烷基酮。这些新抑制剂中最有效的是 4i，其 K(i)为 0.5 μM。这两个系列为 ICE 的疏水面的结合要求提供了更好的理解。
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