Zobrazeno 1 - 10
of 201
pro vyhledávání: '"Carlos A Montanari"'
Autor:
Lorenzo Cianni, Carina Lemke, Erik Gilberg, Christian Feldmann, Fabiana Rosini, Fernanda Dos Reis Rocho, Jean F R Ribeiro, Daiane Y Tezuka, Carla D Lopes, Sérgio de Albuquerque, Jürgen Bajorath, Stefan Laufer, Andrei Leitão, Michael Gütschow, Carlos A Montanari
Publikováno v:
PLoS Neglected Tropical Diseases, Vol 14, Iss 3, p e0007755 (2020)
The cysteine protease cruzipain is considered to be a validated target for therapeutic intervention in the treatment of Chagas disease. A series of 26 new compounds were designed, synthesized, and tested against the recombinant cruzain (Cz) to map it
Externí odkaz:
https://doaj.org/article/3510716dcbcc410e83482bb1244acca6
Publikováno v:
PLoS ONE, Vol 14, Iss 12, p e0222055 (2019)
Cruzain, a cysteine protease of Trypanosoma cruzi, is a validated target for the treatment of Chagas disease. Due to its high similarity in three-dimensional structure with human cathepsins and their sequence identity above 70% in the active site reg
Externí odkaz:
https://doaj.org/article/0a814f2c089a4c8bac5ded449012fd76
Autor:
Antonio C B Burtoloso, Sérgio de Albuquerque, Mark Furber, Juliana C Gomes, Cristiana Gonçalez, Peter W Kenny, Andrei Leitão, Carlos A Montanari, José Carlos Quilles, Jean F R Ribeiro, Josmar R Rocha
Publikováno v:
PLoS Neglected Tropical Diseases, Vol 11, Iss 2, p e0005343 (2017)
The cysteine protease cruzipain is considered to be a validated target for therapeutic intervention in the treatment of Chagas disease. Anti-trypanosomal activity against the CL Brener strain of T. cruzi was observed in the 0.1 μM to 1 μM range for
Externí odkaz:
https://doaj.org/article/c040bb0a668b427ebd712530ad099df5
Autor:
Leandro A A Avelar, Cristian D Camilo, Sérgio de Albuquerque, William B Fernandes, Cristiana Gonçalez, Peter W Kenny, Andrei Leitão, James H McKerrow, Carlos A Montanari, Erika V Meñaca Orozco, Jean F R Ribeiro, Josmar R Rocha, Fabiana Rosini, Marta E Saidel
Publikováno v:
PLoS Neglected Tropical Diseases, Vol 9, Iss 7, p e0003916 (2015)
A series of compounds based on the dipeptidyl nitrile scaffold were synthesized and assayed for their inhibitory activity against the T. cruzi cysteine protease cruzain. Structure activity relationships (SARs) were established using three, eleven and
Externí odkaz:
https://doaj.org/article/c07c0749619b40c0b5dab804ecd2bd13
Autor:
Helton J Wiggers, Josmar R Rocha, William B Fernandes, Renata Sesti-Costa, Zumira A Carneiro, Juliana Cheleski, Albérico B F da Silva, Luiz Juliano, Maria H S Cezari, João S Silva, James H McKerrow, Carlos A Montanari
Publikováno v:
PLoS Neglected Tropical Diseases, Vol 7, Iss 8, p e2370 (2013)
A multi-step cascade strategy using integrated ligand- and target-based virtual screening methods was developed to select a small number of compounds from the ZINC database to be evaluated for trypanocidal activity. Winnowing the database to 23 selec
Externí odkaz:
https://doaj.org/article/f12209661acd4a60a2472e7ba9b7fbeb
Autor:
Vinícius Bonatto, Rafael F. Lameiro, Fernanda R. Rocho, Jerônimo Lameira, Andrei Leitão, Carlos A. Montanari
Publikováno v:
RSC Medicinal Chemistry. 14:201-217
This review highlights the roles of nitriles in covalent inhibitors, their reactivity, examples of pharmaceuticals containing the cyano group and recent developments of nitrile-based inhibitors.
Autor:
Carlos A. Montanari, Rafael da Fonseca Lameiro, Fabiana Rosini, Rodrigo Cendron, Pedro Henrique Jatai Batista, Anwar Shamim
Publikováno v:
Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual)
Universidade de São Paulo (USP)
instacron:USP
Universidade de São Paulo (USP)
instacron:USP
Aim: Compounds that block enzyme activity can kill pathogens and help develop effective and safe drugs for Chagas disease and leishmaniasis. Materials & methods: A library of nonpeptidic nitrile-based compounds was synthesized and had their inhibitor
Autor:
Fernanda R. Rocho, Vinícius Bonatto, Rafael F. Lameiro, Jerônimo Lameira, Andrei Leitão, Carlos A. Montanari
Publikováno v:
Expert opinion on therapeutic patents. 32(5)
Cathepsin K (CatK) is a lysosomal cysteine protease and the predominant cathepsin expressed in osteoclasts, where it degrades the bone matrix. Hence, CatK is an attractive therapeutic target related to diseases characterized by bone resorption, like
Autor:
Alberto M. Dos Santos, Amanda Ruslana Santana Oliveira, Clauber H. S. da Costa, Peter W. Kenny, Carlos A. Montanari, Jaldyr de Jesus G. Varela, Jerônimo Lameira
Publikováno v:
Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual)
Universidade de São Paulo (USP)
instacron:USP
Universidade de São Paulo (USP)
instacron:USP
We have used molecular dynamics (MD) simulations with hybrid quantum mechanics/molecular mechanics (QM/MM) potentials to investigate the reaction mechanism for covalent inhibition of cathepsin K and assess the reversibility of inhibition. The compute
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2f5074cfdea916454354951ad8857eb
Publikováno v:
Letters in Drug Design & Discovery. 17:867-872
Background: Compounds previously studied as anticancer were screened against trypomastigotes to access the bioactivity. The epimastigote form of Trypanosoma cruzi Y strain and the promastigote form of Leishmania amazonensis and Leishmania infantum we