Thirty Years in the Design and Development of Cruzain Inhibitors

Cruzipain is the principal protease of Trypanosoma cruzi, the etiological agent of Chagas disease. Since its discovery in the 1980s and the resolution of the crystal structure of cruzain (a truncated recombinant form of the enzyme) in 1995, this target has attracted the interest of many research gro...

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Autores principales: Jasinski, Gabriel, Martini, M. Florencia, Moglioni, ALbertina
Formato: Artículo de publicación periódica
Lenguaje:Inglés
Publicado: 2024
Materias:
CHAGAS
ENFERMEDAD DE CHAGAS
CRUZAIN
Acceso en línea:https://ri.itba.edu.ar/handle/20.500.14769/4469
Aporte de:
Repositorio Institucional Instituto Tecnológico de Buenos Aires (ITBA) de Instituto Tecnológico de Buenos Aires (ITBA)
id I32-R138-20.500.14769-4469
record_format dspace
spelling I32-R138-20.500.14769-44692026-01-15T14:37:57Z Thirty Years in the Design and Development of Cruzain Inhibitors Jasinski, Gabriel Martini, M. Florencia Moglioni, ALbertina CHAGAS ENFERMEDAD DE CHAGAS CRUZAIN Cruzipain is the principal protease of Trypanosoma cruzi, the etiological agent of Chagas disease. Since its discovery in the 1980s and the resolution of the crystal structure of cruzain (a truncated recombinant form of the enzyme) in 1995, this target has attracted the interest of many research groups for screening studies, structure-based and ligand-based drug design campaigns, which include peptide-like and non-peptide synthetic compounds. In this context, empirical and computational methods have proven to be valuable tools for the study of mechanisms of action, potential binding modes and structure-activity relationships for a diverse series of cruzain/cruzipain inhibitors. This paper, therefore, reviews some of the most relevant chemical groups reported as cruzain inhibitors over the last 30 years of research. 2024-06-13T15:25:03Z 2024-06-13T15:25:03Z 2024-05-03 Artículo de publicación periódica https://ri.itba.edu.ar/handle/20.500.14769/4469 en application/pdf
institution Instituto Tecnológico de Buenos Aires (ITBA)
institution_str I-32
repository_str R-138
collection Repositorio Institucional Instituto Tecnológico de Buenos Aires (ITBA)
language Inglés
topic CHAGAS
ENFERMEDAD DE CHAGAS
CRUZAIN
spellingShingle CHAGAS
ENFERMEDAD DE CHAGAS
CRUZAIN
Jasinski, Gabriel
Martini, M. Florencia
Moglioni, ALbertina
Thirty Years in the Design and Development of Cruzain Inhibitors
topic_facet CHAGAS
ENFERMEDAD DE CHAGAS
CRUZAIN
description Cruzipain is the principal protease of Trypanosoma cruzi, the etiological agent of Chagas disease. Since its discovery in the 1980s and the resolution of the crystal structure of cruzain (a truncated recombinant form of the enzyme) in 1995, this target has attracted the interest of many research groups for screening studies, structure-based and ligand-based drug design campaigns, which include peptide-like and non-peptide synthetic compounds. In this context, empirical and computational methods have proven to be valuable tools for the study of mechanisms of action, potential binding modes and structure-activity relationships for a diverse series of cruzain/cruzipain inhibitors. This paper, therefore, reviews some of the most relevant chemical groups reported as cruzain inhibitors over the last 30 years of research.
format Artículo de publicación periódica
author Jasinski, Gabriel
Martini, M. Florencia
Moglioni, ALbertina
author_facet Jasinski, Gabriel
Martini, M. Florencia
Moglioni, ALbertina
author_sort Jasinski, Gabriel
title Thirty Years in the Design and Development of Cruzain Inhibitors
title_short Thirty Years in the Design and Development of Cruzain Inhibitors
title_full Thirty Years in the Design and Development of Cruzain Inhibitors
title_fullStr Thirty Years in the Design and Development of Cruzain Inhibitors
title_full_unstemmed Thirty Years in the Design and Development of Cruzain Inhibitors
title_sort thirty years in the design and development of cruzain inhibitors
publishDate 2024
url https://ri.itba.edu.ar/handle/20.500.14769/4469
work_keys_str_mv AT jasinskigabriel thirtyyearsinthedesignanddevelopmentofcruzaininhibitors
AT martinimflorencia thirtyyearsinthedesignanddevelopmentofcruzaininhibitors
AT moglionialbertina thirtyyearsinthedesignanddevelopmentofcruzaininhibitors
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