新型基于酒石酸盐的 TNF-α转化酶（TACE）抑制剂的发现。
The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors.
机构信息
Department of Medicinal Chemistry, Schering-Plough Research Institute Cambridge, 320 Bent Street, Cambridge, MA 02141, United States.
出版信息
Bioorg Med Chem Lett. 2010 Feb 1;20(3):1189-93. doi: 10.1016/j.bmcl.2009.12.004. Epub 2009 Dec 5.
PMID:20022498
Abstract
A novel series of TNF-alpha convertase (TACE) inhibitors which are non-hydroxamate have been discovered. These compounds are bis-amides of L-tartaric acid (tartrate) and coordinate to the active site zinc in a tridentate manner. They are selective for TACE over other MMP's. We report the first X-ray crystal structure for a tartrate-based TACE inhibitor.
摘要
现已发现一系列新型 TNF-α 转化酶（TACE）抑制剂，它们均不属于羟胺类。这些化合物是 L-酒石酸（酒石酸盐）的双酰胺，以三齿配位方式与活性部位锌配位。它们对 TACE 的选择性高于其他 MMP。我们报告了首个基于酒石酸盐的 TACE 抑制剂的 X 射线晶体结构。
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