Gawlik Katarzyna, Poreba Wojciech, Gutowicz Jan
Zaklład Fizykochemii Drobnoustrojów, Instytut Genetyki i Mikrobiologii, Uniwersytet Wrocławski, Wrocław.
Postepy Biochem. 2005;51(3):318-27.
Protein inhibitors of proteolytic enzymes play an important role in regulating the activity of endogenous proteases and in host defense mechanisms against pathogens preventing the deleterious effects of exogenous proteases. In recent years a great interest in protein inhibitors of cysteine proteases has increased due to the extensive growth of knowledge about the contribution of cysteine proteases to pathological processes associated with many human diseases, as well as due to prospects for treatment of these disorders which may arise from the thorough understanding of their inhibitory mechanisms. This paper reviews the most important aspects of three families of cysteine protease inhibitors: cystatins, thyropins and inhibitors homologous to propeptides of cysteine proteases. Special attention is given to structural bases of the interactions between the inhibitors and their target enzymes. The paper presents a general characterization of the families according to the MEROPS classification of protease inhibitors, pointing out new members.
蛋白水解酶的蛋白质抑制剂在调节内源性蛋白酶活性以及宿主抵御病原体的防御机制中发挥着重要作用,可防止外源性蛋白酶的有害影响。近年来,由于对半胱氨酸蛋白酶在许多人类疾病相关病理过程中的作用的认识不断深入,以及对这些疾病治疗前景的展望(这可能源于对其抑制机制的深入理解),人们对半胱氨酸蛋白酶的蛋白质抑制剂产生了浓厚兴趣。本文综述了半胱氨酸蛋白酶抑制剂三个家族的最重要方面:胱抑素、甲状腺素结合球蛋白以及与半胱氨酸蛋白酶前肽同源的抑制剂。特别关注了抑制剂与其靶酶相互作用的结构基础。本文根据蛋白酶抑制剂的MEROPS分类对这些家族进行了总体描述,并指出了新成员。