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Cysteine proteases as potential targets for anti-trypanosomatid drug discovery
Bioorganic & Medicinal Chemistry ( IF 3.5 ) Pub Date : 2021-08-13 , DOI: 10.1016/j.bmc.2021.116365
Wagner A S Judice 1 , Letícia Silva Ferraz 2 , Rayssa de Mello Lopes 2 , Luan Dos Santos Vianna 1 , Fábio da Silva Siqueira 1 , Juliana F Di Iorio 1 , Laura de Azevedo Maffeis Dalzoto 1 , Mariana Nascimento Romero Trujilho 1 , Taiz Dos Reis Santos 1 , Maurício F M Machado 1 , Tiago Rodrigues 2
Affiliation  

Leishmaniasis and trypanosomiasis are endemic neglected disease in South America and Africa and considered a significant public health problem, mainly in poor communities. The limitations of the current available therapeutic options, including the lack of specificity, relatively high toxicity, and the drug resistance acquiring, drive the constant search for new targets and therapeutic options. Advances in knowledge of parasite biology have revealed essential enzymes involved in the replication, survival, and pathogenicity of Leishmania and Trypanosoma species. In this scenario, cysteine proteases have drawn the attention of researchers and they are being proposed as promising targets for drug discovery of antiprotozoal drugs. In this systematic review, we will provide an update on drug discovery strategies targeting the cysteine proteases as potential targets for chemotherapy against protozoal neglected diseases.



中文翻译:

半胱氨酸蛋白酶作为抗锥虫药物发现的潜在靶点

利什曼病和锥虫病是南美洲和非洲的地方性被忽视疾病,被认为是一个重大的公共卫生问题,主要发生在贫困社区。当前可用治疗方案的局限性,包括缺乏特异性、相对较高的毒性和耐药性的获得,推动了对新靶点和治疗方案的不断探索。寄生虫生物学知识的进步揭示了参与利什曼原虫锥虫复制、存活和致病性的必需酶物种。在这种情况下,半胱氨酸蛋白酶引起了研究人员的注意,它们被提议作为抗原生动物药物药物发现的有希望的靶点。在这篇系统综述中,我们将提供针对半胱氨酸蛋白酶作为针对原生动物被忽视疾病的化疗的潜在靶点的药物发现策略的更新。

更新日期:2021-08-20
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