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Abstract：
BACKGROUND: Cathepsins play an important role in protein degradation and processing. Aberrant cathepsin B or L is closely associated with many serious diseases such as cancer, osteoporosis and autoimmune disorders. Therefore, development of potent and selective cathepsin B and L inhibitors has aroused much attention in recent years. Although several classes of cathepsin inhibitors are presently available, there are still some problems to solve, such as broad-spectrum inhibition to protease, specially cysteine proteases, which lead to unpredictable side effects in clinical trials. Therefore, it is very necessary to discovery new scaffolds and new application of cathepsin B and L inhibitors for developing therapeutic agents for treating diseases mediated by cathepsin B or L. Areas covered: This updated review summarizes new patents on cathepsin B and L inhibitors from 2010 to present. Expert opinion: The review gives the latest development in the area of inhibitors of cathepsin B and L, which have been considered key therapeutic targets for the development of drugs treating related diseases. This review puts emphasis on the discovery of novel small molecule inhibitors of cathepsin B and L, as well as their new application as new therapeutic agents.
摘要：
背景：组织蛋白酶在蛋白质降解和加工中起重要作用。异常组织蛋白酶B或L与许多严重疾病如癌症密切相关,骨质疏松症和自身免疫性疾病。因此,近年来，高效、选择性的组织蛋白酶B和L抑制剂的开发引起了人们的广泛关注。尽管目前有几类组织蛋白酶抑制剂，还有一些问题需要解决，例如对蛋白酶的广谱抑制，特别是半胱氨酸蛋白酶，导致临床试验中不可预测的副作用。因此,非常有必要发现组织蛋白酶B和L抑制剂的新支架和新应用，以开发治疗由组织蛋白酶B或L介导的疾病的治疗剂。涵盖的领域：这篇最新综述总结了2010年至今关于组织蛋白酶B和L抑制剂的新专利。专家意见：这篇综述给出了组织蛋白酶B和L抑制剂领域的最新进展，已被认为是治疗相关疾病的药物开发的关键治疗靶标。本文重点介绍了组织蛋白酶B和L的新型小分子抑制剂的发现。以及它们作为新治疗剂的新应用。
