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小分子肽酶荧光探针设计策略。

Strategies in the design of small-molecule fluorescent probes for peptidases.

机构信息

Key Laboratory of Chemical Biology (MOE), Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Jinan, China.

出版信息

Med Res Rev. 2014 Nov;34(6):1217-41. doi: 10.1002/med.21316. Epub 2014 Apr 14.

DOI:10.1002/med.21316
PMID:24733434
Abstract

Peptidases, which can cleave specific peptide bonds in innumerable categories of substrates, usually present pivotal positions in protein activation, cell signaling and regulation as well as in the origination of amino acids for protein generation or application in other metabolic pathways. They are also involved in many pathological conditions, such as cancer, atherosclerosis, arthritis, and neurodegenerative disorders. This review article aims to conduct a wide-ranging survey on the development of small-molecule fluorescent probes for peptidases, as well as to realize the state of the art in the tailor-made probes for diverse types of peptidases.

摘要

肽酶可以切割无数种类底物中的特定肽键,通常在蛋白质激活、细胞信号转导和调控以及氨基酸生成用于蛋白质产生或应用于其他代谢途径中起着关键作用。它们还与许多病理状况有关,如癌症、动脉粥样硬化、关节炎和神经退行性疾病。本文综述了肽酶小分子荧光探针的发展,并实现了针对不同类型肽酶的定制探针的最新技术状态。

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Strategies in the design of small-molecule fluorescent probes for peptidases.小分子肽酶荧光探针设计策略。
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A robust, high-sensitivity stealth probe for peptidases.一种稳健、高灵敏度的肽酶隐身探针。
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Recent advances and concepts in substrate specificity determination of proteases using tailored libraries of fluorogenic substrates with unnatural amino acids.使用含非天然氨基酸的荧光底物定制文库测定蛋白酶底物特异性的最新进展和概念。
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Applications for chemical probes of proteolytic activity.蛋白水解活性化学探针的应用。
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Chemical probes shed light on protein function.化学探针有助于揭示蛋白质的功能。
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