Cruzain
Mostrando 1-11 de 11 artigos, teses e dissertações.
-
1. Agradecimentos aos Pareceristas ad hoc do volume 18 (ano 2020)
According to the World Health Organization (WHO), Chagas disease (CD), whose etiological agent is the Trypanosoma cruzi (T. cruzi) parasite, affects about eight million people, mainly in Latin America. The cruzain enzyme is highlighted among the main biological targets, since it is the most abundant of the cysteine protease class from T. cruzi and is involve
Trab. educ. saúde. Publicado em: 2021-01
-
2. Molecular Modelling Study of Heteroarylamide/Sulfonamide Compounds with Antitrypanosomal Activity
According to the World Health Organization (WHO), Chagas disease (CD), whose etiological agent is the Trypanosoma cruzi (T. cruzi) parasite, affects about eight million people, mainly in Latin America. The cruzain enzyme is highlighted among the main biological targets, since it is the most abundant of the cysteine protease class from T. cruzi and is involve
J. Braz. Chem. Soc.. Publicado em: 2021-01
-
3. An in silico Study of Benzophenone Derivatives as Potential Non-Competitive Inhibitors of Trypanosoma cruzi and Leishmania Amazonensis Cysteine Proteinases
This study investigates the mechanisms of interaction between benzophenone derivatives and cruzain and Llacys1 (the protein expressed by cysteine protease gene isoform 1 of L. amazonensis) by homology modelling, docking and molecular dynamics simulation. The results predict that the same binding site in cruzain and Llacys1 is involved in complexes with benzo
J. Braz. Chem. Soc.. Publicado em: 2018-03
-
4. Identificação de novos inibidores da enzima cruzaína de Trypanosoma cruzi candidatos a fármacos contra a doença de Chagas / Discovery of novel inhibitors of the cruzain enzyme from Trypanosoma cruzi as drug candidates against Chagas disease
A doença de Chagas, uma infecção parasitária amplamente distribuída na América Latina, é um problema grave de saúde pública com consequências devastadoras em termos de morbidade e mortalidade humana. O arsenal terapêutico contra a doença é bastante limitado e insuficiente em todos os aspectos clínicos. Visando o desenvolvimento de novos agentes
IBICT - Instituto Brasileiro de Informação em Ciência e Tecnologia. Publicado em: 30/07/2012
-
5. Planejamento de inibidores da cruzaína baseado em fragmentos / Fragment based drug design of cruzain inhibitors
A Doença de Chagas, descrita em 1909 pelo médico sanitarista brasileiro Dr. Carlos Chagas, é causada pelo parasito tripanossomatídeo Trypanosoma cruzi. Os tratamentos atuais consistem no uso dos fármacos benzonidazol e nifurtimox que são eficazes apenas no estágio inicial da doença (fase aguda), mas possuem efeitos colaterais severos. A enzima cruza�
IBICT - Instituto Brasileiro de Informação em Ciência e Tecnologia. Publicado em: 27/07/2011
-
6. Biochemical evaluation of a series of synthetic chalcone and hydrazide derivatives as novel inhibitors of cruzain from Trypanosoma cruzi
A doença de Chagas, uma infecção parasitária amplamente distribuída na América Latina, é um problema grave de saúde pública com conseqüências devastadoras em termos de morbidade e mortalidade humana. A enzima cruzaína é a principal cisteíno protease do Trypanosoma cruzi, agente etiológico da tripanossomíase Americana ou doença de Chagas, e f
Journal of the Brazilian Chemical Society. Publicado em: 2010
-
7. Two approaches to discovering and developing new drugs for Chagas disease
This review will focus on two general approaches carried out at the Sandler Center, University of California, San Francisco, to address the challenge of developing new drugs for the treatment of Chagas disease. The first approach is target-based drug discovery, and two specific targets, cytochrome P450 CYP51 and cruzain (aka cruzipain), are discussed. A "pro
Memórias do Instituto Oswaldo Cruz. Publicado em: 2009-07
-
8. SÃntese e avaliaÃÃo de tiossemicarbazonas e tiazolinonas como inibidores da protease cruzaÃna do Trypanosoma cruzi
Chagas disease is still a specific and impressive problem in Latin America, under many aspects linked to questions related to social inequity and globalization process. The disease, in spite of financial and policies difficulties, has been controlled; however, a period of two or three decades remains necessary for the consolidation of control, surveillance i
Publicado em: 2008
-
9. Study of physiochemical properties and criteria for obtaining and validation of QSAR models of similar semicarbazonas set with antichagasic activity, selected of literature / Estudo de propriedades físico-químicas e de critérios para obtenção e validação de modelos QSAR para séries de análogos de semicarbazonas com atividade antichagásica, retiradas da literatura
It has been observed an enormous improvement in the methods concerning data generation, leading to a large amount of information, especially for chemical and biological systems. Through these developments, it becomes relevant to have reliable methods, mainly new mathematical tools, for structure-activity relationship (SAR) data examination, which means that
Publicado em: 2005
-
10. Vinyl Sulfones as Antiparasitic Agents and a Structural Basis for Drug Design*
Cysteine proteases of the papain superfamily are implicated in a number of cellular processes and are important virulence factors in the pathogenesis of parasitic disease. These enzymes have therefore emerged as promising targets for antiparasitic drugs. We report the crystal structures of three major parasite cysteine proteases, cruzain, falcipain-3, and th
American Society for Biochemistry and Molecular Biology.
-
11. Rapid and general profiling of protease specificity by using combinatorial fluorogenic substrate libraries
A method is presented for the preparation and use of fluorogenic peptide substrates that allows for the configuration of general substrate libraries to rapidly identify the primary and extended specificity of proteases. The substrates contain the fluorogenic leaving group 7-amino-4-carbamoylmethylcoumarin (ACC). Substrates incorporating the ACC leaving group
The National Academy of Sciences.