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Cathepsin-sensitive nanoscale drug delivery systems for cancer therapy and other diseases

机译：表达敏感纳米级药物递送系统，用于癌症治疗和其他疾病

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摘要

Cathepsins are an important category of enzymes that have attracted great attention for the delivery of drugs to improve the therapeutic outcome of a broad range of nanoscale drug delivery systems. These proteases can be utilized for instance through actuation of polymer-drug conjugates (e.g., triggering the drug release) to bypass limitations of many drug candidates. A substantial amount of work has been witnessed in the design and the evaluation of Cathepsin-sensitive drug delivery systems, especially based on the tetra-peptide sequence (Gly-Phe-Leu-Gly, GFLG) which has been extensively used as a spacer that can be cleaved in the presence of Ca-thepsin B. This Review Article will give an in-depth overview of the design and the biological evaluation of Cathepsin-sensitive drug delivery systems and their application in different pathologies including cancer before discussing Cathepsin B-cleavable prodrugs under clinical trials.
机译：组织汀是一种重要的酶类别，它引起了备受关注的药物，以改善广泛的纳米级药物递送系统的治疗结果。 这些蛋白酶可以通过致动聚合物 - 药物缀合物（例如，引发药物释放）来绕过许多毒品候选物的限制。 在设计和对组织素敏感药物输送系统的设计和评估中有大量的作品，特别是基于已经广泛用作间隔物的四肽序列（Gly-Phe-Leu-Gly，GFLG） 可以在Ca-Thepsin B的存在下切割。该审查制品将深入概述组织素敏感药物递送系统的设计和生物学评估及其在包括癌症的不同病程中的应用，然后讨论组织蛋白酶B可释放 临床试验下的前药。

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