Instituto de Química, Universidad Nacional Autónoma de México, Av. Universidad 3000, Mexico City 04510, Mexico.
The University of Alabama in Huntsville, Huntsville, AL 35899, USA.
Drug Discov Today. 2015 Jul;20(7):890-8. doi: 10.1016/j.drudis.2015.02.004. Epub 2015 Feb 16.
Human African trypanosomiasis and Chagas disease are the main causes of heart failure in developing countries. The disadvantages of current therapy include: undesirable side-effects, resistance, lack of efficacy on late-stage disease and lack of pediatric formulations. Efforts to find new compound hits have spanned SAR studies to very high-throughput and virtual screens and drug repurposing. The integrated analysis of these strategies on the discovery of anti-Chagas agents is timely. This work accounts for the progress on the development of cruzain inhibitors following these avenues, with emphasis on structural aspects of the ligand-cruzain recognition process.
人类非洲锥虫病和恰加斯病是发展中国家心力衰竭的主要原因。目前治疗方法的缺点包括：副作用不理想、耐药性、对晚期疾病疗效不佳以及缺乏儿科制剂。寻找新的化合物的努力涵盖了 SAR 研究、高通量筛选和虚拟筛选以及药物再利用。及时对这些策略在抗恰加斯病药物发现中的综合分析。这项工作描述了在这些途径下开发克氏锥虫抑制剂的进展，重点是配体与克氏锥虫识别过程的结构方面。
