摘要
查加斯氏病是在美洲影响最大和最流行的被忽视的热带疾病之一,特别影响着拉丁美洲贫穷和不发达地区。治疗该疾病的慢性阶段中化学疗法使用的药物比较陈旧,有毒且呈现较低疗效,也恶化这种病情。另外,病原体克氏锥虫耐药菌株也经常被报道。因此,为治疗这种衰竭性疾病,新的化学疗法的选择需求也是势在必行。在这种背景下,肽酶作为一种潜在的靶制剂出现,因此,蛋白酶抑制剂已经被证实为抵抗一些人类病理的有价值药物。依照这种思路,克氏锥虫产生了多功能的半胱氨酸肽酶,命名为cruzipain,其直接和/或间接地调控一些病理和生理过程,以成功感染寄生虫为终结。总之,这些调查结果指出cruzipain是驾驭 抗人类病原体克氏锥虫化学疗法方案的最重要的靶点之一。该综述着重于近期发表的研究,总结了该领域的近期研究进展及失败。
关键词: 查加斯氏病,克氏锥虫,人类病原体,被忽视的热带疾病,半胱氨酸肽酶,cruzipain,蛋白酶抑制剂,化学疗法
Current Medicinal Chemistry
Title:Cruzipain: An Update on its Potential as Chemotherapy Target against the Human Pathogen Trypanosoma cruzi
Volume: 22 Issue: 18
Author(s): M.H. Branquinha, S.S.C. Oliveira, L.S. Sangenito, C.L. Sodre, L.F. Kneipp, C.M. d’Avila-Levy and A.L.S. Santos
Affiliation:
关键词: 查加斯氏病,克氏锥虫,人类病原体,被忽视的热带疾病,半胱氨酸肽酶,cruzipain,蛋白酶抑制剂,化学疗法
摘要: Chagas’ disease is one of the most impactful and prevalent neglected tropical diseases in the Americas, specially affecting the poor and underdeveloped areas in Latin America. Aggravating this scenario, the medicines used in the current chemotherapy are old, toxic and present a low efficacy to treat the chronic stage of this disease. In addition, resistant strains of Trypanosoma cruzi, the etiological agent, are frequently reported. So, there is an imperative requirement for novel chemotherapeutic options to treat this debilitating disease. In this context, peptidases have emerged as potential targets and, consequently, proteolytic inhibitors have confirmed to be valuable drugs against several human pathologies. In this line of thinking, T. cruzi produces a major multifunctional cysteine peptidase, named cruzipain, which directly and/or indirectly orchestrates several physiological and pathological processes, which culminate in a successful parasitic infection. Taken together, these findings point out that cruzipain is one of the most important targets for driving a chemotherapy approach against the human pathogen T. cruzi. The present review summarizes some of the recent advances and failures in this area, with particular emphasis on recently published studies.
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M.H. Branquinha, S.S.C. Oliveira, L.S. Sangenito, C.L. Sodre, L.F. Kneipp, C.M. d’Avila-Levy and A.L.S. Santos , Cruzipain: An Update on its Potential as Chemotherapy Target against the Human Pathogen Trypanosoma cruzi, Current Medicinal Chemistry 2015; 22 (18) . https://dx.doi.org/10.2174/0929867322666150521091652
DOI https://dx.doi.org/10.2174/0929867322666150521091652 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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