Kallikrein‐related peptidases (KLKs) are a family of 15 secreted serine proteases that are involved in various physiological processes. Their activities are subtly regulated by various endogenous inhibitors, ranging from metallic ions to macromolecular entities such as proteins. Furthermore, dysregulation of KLK activity has been linked to several pathologies, including cancer and skin and inflammatory diseases, explaining the numerous efforts to develop KLK‐specific pharmacological inhibitors as potential therapeutic agents. In this review, we focus on the huge repertoire of KLKs inhibitors reported to date with a special emphasis on the diversity of their molecular mechanisms of inhibition.

中文翻译：

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激肽释放酶相关肽酶的抑制剂：概述

激肽释放酶相关肽酶（KLK）是15种分泌的丝氨酸蛋白酶家族，涉及各种生理过程。它们的活性受到各种内源性抑制剂（从金属离子到大分子实体，例如蛋白质）的调节。此外，KLK活性失调与多种病理学有关，包括癌症，皮肤病和炎性疾病，这解释了为开发KLK特异性药理抑制剂作为潜在治疗剂而付出的巨大努力。在这篇综述中，我们集中于迄今为止报道的大量KLKs抑制剂，特别着重于其抑制分子机制的多样性。