Abstract
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.
Keywords: Chagas’ disease, Trypanosoma cruzi, human pathogen, neglected tropical disease, cysteine peptidases, cruzipain, proteolytic inhibitors, chemotherapy.
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:
Keywords: Chagas’ disease, Trypanosoma cruzi, human pathogen, neglected tropical disease, cysteine peptidases, cruzipain, proteolytic inhibitors, chemotherapy.
Abstract: 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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Branquinha M.H., Oliveira S.S.C., Sangenito L.S., Sodre C.L., Kneipp L.F., d’Avila-Levy C.M. and Santos A.L.S., 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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