Synthesis and structure activity relationships of novel small molecule cathepsin D inhibitors
Synthesis and structure activity relationships of novel small molecule cathepsin D inhibitors
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DOI：
10.1016/s0960-894x(99)00433-3
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发表时间：
1999-09-06
影响因子：
2.7
通讯作者：
Wong, S
中科院分区：
文献类型：
--
作者：
Dumas, J;Brittelli, D;Wong, S
组织蛋白酶D是一种溶酶体乙酰化蛋白酶，与阿尔茨海默病以及乳腺癌和卵巢癌的病理学有关。通过高通量筛选鉴定了弱活性的组织蛋白酶D抑制剂。随后的优化导致发现了这种酶的一类新的小分子抑制剂，最终发现了磺酰胺13（IC50 = 250 nM），（C）1999 Elsevier Science Ltd.保留所有权利。
Cathepsin D, a lysosomal aspartyl protease, has been implicated in the pathology of Alzheimer's disease as well as breast and ovarian cancer. A weakly active cathepsin D inhibitor was identified by high throughput screening. Subsequent optimization led to the discovery of a new class of small molecule inhibitors of this enzyme, culminating with the sulfonamide 13 (IC50 = 250 nM), (C) 1999 Elsevier Science Ltd. All rights reserved.