University of Nottingham, School of Molecular Medical Sciences, Nottingham NG5 1PB, UK.
Nat Rev Cancer. 2011 May;11(5):364-74. doi: 10.1038/nrc3050.
The calpains are a conserved family of cysteine proteinases that catalyse the controlled proteolysis of many specific substrates. Calpain activity is implicated in several fundamental physiological processes, including cytoskeletal remodelling, cellular signalling, apoptosis and cell survival. Calpain expression is altered during tumorigenesis, and the proteolysis of numerous substrates, such as inhibitors of nuclear factor-κB (IκB), focal adhesion proteins (including, focal adhesion kinase and talin) and proto-oncogenes (for example, MYC), has been implicated in tumour pathogenesis. Recent evidence indicates that the increased expression of certain family members might influence the response to cancer therapies, providing justification for the development of novel calpain inhibitors.
钙蛋白酶是一类保守的半胱氨酸蛋白酶家族，能够催化许多特定底物的可控蛋白水解。钙蛋白酶活性与几种基本的生理过程有关，包括细胞骨架重塑、细胞信号转导、细胞凋亡和细胞存活。在肿瘤发生过程中，钙蛋白酶的表达发生改变，并且许多底物（如核因子-κB（NF-κB）抑制剂 IκB、细胞黏附蛋白（包括黏着斑激酶和桩蛋白）和原癌基因（如 MYC））的蛋白水解与肿瘤发病机制有关。最近的证据表明，某些家族成员的表达增加可能会影响对癌症治疗的反应，这为开发新型钙蛋白酶抑制剂提供了依据。
