Unidade de Tecnologias de Proteínas e Anticorpos Monoclonais, Instituto de Higiene e Medicina Tropical, Lisboa, Portugal.
Transbound Emerg Dis. 2010 Apr;57(1-2):68-9. doi: 10.1111/j.1865-1682.2010.01102.x.
Papain-like cysteine proteases (CP) have been shown to have essential roles in parasitic protozoa and are under study as promising drug targets. One gene was identified by sequence similarity search to be homologous to the CP family in the ongoing Babesia bigemina genome sequencing project database. The newly identified CP gene, called babesipain-1, was cloned and expressed as a fusion protein, and the effect of different inhibitors on proteolytic activity was tested. A series of new artemisinin-vinyl sulfone hybrid molecules were tested as inhibitors being effective on the range of 0.3-30 microm, depending on the core-containing molecule.
木瓜样半胱氨酸蛋白酶（CP）已被证明在寄生原生动物中具有重要作用，并作为有前途的药物靶点进行研究。在正在进行的巴贝西虫全基因组测序项目数据库中，通过序列相似性搜索鉴定出一个与 CP 家族同源的基因。新鉴定的 CP 基因，称为 babesipain-1，被克隆并表达为融合蛋白，并测试了不同抑制剂对蛋白水解活性的影响。一系列新的青蒿素-乙烯砜杂合分子被测试为抑制剂，其有效浓度范围为 0.3-30μm，具体取决于含核分子。
