McKerrow J H
Department of Pathology, UCSF/VA Medical Center, San Francisco, CA 94121, USA.
Int J Parasitol. 1999 Jun;29(6):833-7. doi: 10.1016/s0020-7519(99)00044-2.
Cysteine proteases have been identified as promising targets for the development of antiparasitic chemotherapy. An attractive aspect of these enzymes is their widespread importance in both protozoan and helminth parasites of domestic animals and humans. Concerns about the ability to selectively inhibit parasite proteases without affecting host homologues have been addressed in recent studies of Trypanosoma cruzi and Plasmodium falciparum. Significant data on half-life, metabolism, pharmacokinetics and safety have been accumulated. Differential uptake of proteases by parasitic organisms versus host cells, and relatively less redundancy in parasite protease gene families, may be two factors which contribute to the successful treatment of animal models of infection.
半胱氨酸蛋白酶已被确定为抗寄生虫化疗药物开发的有前景的靶点。这些酶的一个吸引人的方面是它们在家畜和人类的原生动物及蠕虫寄生虫中都具有广泛的重要性。在最近对克氏锥虫和恶性疟原虫的研究中，已经解决了关于选择性抑制寄生虫蛋白酶而不影响宿主同源物的能力的问题。已经积累了关于半衰期、代谢、药代动力学和安全性的大量数据。寄生生物与宿主细胞对蛋白酶的不同摄取，以及寄生虫蛋白酶基因家族中相对较少的冗余，可能是有助于成功治疗感染动物模型的两个因素。
