CRUZAIN The Path from Target Validation to the Clinic
CRUZAIN The Path from Target Validation to the Clinic
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DOI：
10.1007/978-1-4419-8414-2_7
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发表时间：
2011-01-01
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影响因子：
--
通讯作者：
McKerrow, James H.
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文献类型：
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作者：
Sajid, Mohammed;Robertson, Stephanie A.;McKerrow, James H.
克鲁赞酶是克氏锥虫的主要木瓜蛋白酶样半胱氨酸蛋白酶，是南美洲人类查加斯病的病原体。Cruzain对于这种原生动物寄生虫的生存和繁殖是不可或缺的，因此，它作为潜在的药物靶标引起了人们的极大兴趣。本章描绘了从最初鉴定这种蛋白酶的活性并将其作为骨药物靶标的验证，到发现针对这种蛋白酶的抑制剂的艰巨任务，最后走向临床的道路。
Cruzain is the major papain-like cysteine protease of Trypanosoma cruzi, the etiological agent causing Chagas' disease in humans in South America. Cruzain is indispensable for the survival and propagation of this protozoan parasite and therefore, it has attracted considerable interest as a potential drug target. This chapter charts the path from the initial identification of this proteases activity and its validation as a bone fide drug target to the arduous task of the discovery of an inhibitor targeting this protease and finally the path towards the clinic.