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溶酶体半胱氨酸蛋白酶:组织蛋白酶的结构、功能及抑制作用

Lysosomal cysteine proteases: structure, function and inhibition of cathepsins.

作者信息

Roberts Rebecca

机构信息

Department of Biology and Program in Biochemistry and Molecular Biology, Ursinus College, Collegeville, PA 19426, USA.

出版信息

Drug News Perspect. 2005 Dec;18(10):605-14. doi: 10.1358/dnp.2005.18.10.949485.

Abstract

Lysosomal cysteine proteases, a subgroup of the cathepsin family, are critical for normal cellular functions such as general protein turnover, antigen processing and bone remodeling. In the past decade, the number of identified human cathepsins has more than doubled and their known role in several pathologies has expanded rapidly. Increased understanding of the structure and mechanism of this class of enzymes has brought on a new fervor in the design of small molecule inhibitors with the hope of producing specific, therapeutic drugs for diseases such as arthritis, allergy, multiple sclerosis, atherosclerosis, Alzheimer's disease and cancer.

摘要

溶酶体半胱氨酸蛋白酶是组织蛋白酶家族的一个亚群,对于正常细胞功能至关重要,如一般蛋白质周转、抗原加工和骨重塑。在过去十年中,已鉴定出的人类组织蛋白酶数量增加了一倍多,并且它们在几种病理状况中的已知作用迅速扩大。对这类酶的结构和机制的深入了解激发了设计小分子抑制剂的新热潮,希望能生产出针对关节炎、过敏、多发性硬化症、动脉粥样硬化、阿尔茨海默病和癌症等疾病的特异性治疗药物。

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