Search Results - "Rodrigues, Valnês S."

Design of Novel Inhibitors of Human Thymidine Phosphorylase: Synthesis, Enzyme Inhibition, in Vitro Toxicity, and Impact on Human Glioblastoma Cancer by de Moura Sperotto, Nathalia D, Deves Roth, Candida, Rodrigues-Junior, Valnês S, Ev Neves, Christiano, Reisdorfer Paula, Fávero, da Silva Dadda, Adilio, Bergo, Pedro, Freitas de Freitas, Talita, Souza Macchi, Fernanda, Moura, Sidnei, Duarte de Souza, Ana Paula, Campos, Maria Martha, Valim Bizarro, Cristiano, Santos, Diógenes Santiago, Basso, Luiz Augusto, Machado, Pablo

“…Overexpressed human thymidine phosphorylase (hTP) has been associated with cancer aggressiveness and poor prognosis by triggering proangiogenic and…”
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Inhibitory activity of pentacyano(isoniazid)ferrate(II), IQG-607, against promastigotes and amastigotes forms of Leishmania braziliensis by Amorim, Camila F, Galina, Luiza, Carvalho, Natália B, Sperotto, Nathalia D M, Pissinate, Kenia, Machado, Pablo, Campos, Maria M, Basso, Luiz A, Rodrigues-Junior, Valnês S, Carvalho, Edgar M, Santos, Diógenes Santiago

“…M. tuberculosis and parasites of the genus Leishmania present the type II fatty acid biosynthesis system (FASII). The pentacyano(isoniazid)ferrate(II)…”
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Functional, thermodynamics, structural and biological studies of in silico-identified inhibitors of Mycobacterium tuberculosis enoyl-ACP(CoA) reductase enzyme by Martinelli, Leonardo K. B., Rotta, Mariane, Villela, Anne D., Rodrigues-Junior, Valnês S., Abbadi, Bruno L., Trindade, Rogério V., Petersen, Guilherme O., Danesi, Giuliano M., Nery, Laura R., Pauli, Ivani, Campos, Maria M., Bonan, Carla D., de Souza, Osmar Norberto, Basso, Luiz A., Santos, Diogenes S.

“…Novel chemotherapeutics agents are needed to kill Mycobacterium tuberculosis , the main causative agent of tuberculosis (TB). The M. tuberculosis 2- tran…”
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Four diterpenes identified in silico were isolated from Hyptidinae and demonstrated in vitro activity against Mycobacterium tuberculosis by Cavalcanti, Andreza Barbosa Silva, Maia, Mayara dos Santos, Figueiredo, Pedro Thiago Ramalho de, Menezes, Renata Priscila Barros de, Monteiro, Alex France Messias, Meireles, Roseana Araújo Ramos, Rodrigues, Gabriela Cristina Soares, Rodrigues de Almeida Silva, Ana Rita, Lins, Jociano da Silva, Cordeiro, Laísa Vilar, Junior, Valnês S. Rodrigues, Castelo Branco, Ana Paula O. T., Agra, Maria de Fátima, Sessions, Zoe L., Muratov, Eugene N., Scotti, Luciana, Silva, Marcelo Sobral da, Costa, Vicente Carlos de Oliveira, Tavares, Josean Fechine, Scotti, Marcus Tullius

“…Plants of Hyptidinae subtribe (Lamiaceae - family), as Mesosphaerum sidifolium, are a source of bioactive molecules. In the search for new drug candidates, we…”
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Construction of Mycobacterium tuberculosis cdd knockout and evaluation of invasion and growth in macrophages by Villela, Anne Drumond, Rodrigues-Junior, Valnês S, Pinto, Antônio Frederico Michel, Falcão, Virgínia Carla de Almeida, Sánchez-Quitian, Zilpa Adriana, Eichler, Paula, Bizarro, Cristiano Valim, Basso, Luiz Augusto, Santos, Diógenes Santiago

“…Cytidine deaminase (MtCDA), encoded by cdd gene (Rv3315c), is the only enzyme identified in nucleotide biosynthesis pathway of Mycobacterium tuberculosis that…”
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Targeting thymidine phosphorylase inhibition in human colorectal cancer xenografts by Sperotto, Nathalia D. de Moura, Silva, Rodrigo Braccini Madeira, Perelló, Marcia Alberton, Borsoi, Ana Flávia, da Silva Dadda, Adilio, Roth, Candida Deves, Freitas, Raquel Dal Sasso, de Souza, Ana Paula Duarte, Freitas, Deise do Nascimento de, Picada, Jaqueline Nascimento, de Sousa, Jayne Torres, Nabinger, Débora Dreher, Altenhofen, Stefani, Bonan, Carla Denise, Rodrigues-Junior, Valnês S., Bizarro, Cristiano Valim, Basso, Luiz Augusto, Machado, Pablo

“…Human thymidine phosphorylase (hTP) is overexpressed in several solid tumors and is commonly associated with aggressiveness and unfavorable prognosis…”
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DITERPENOS ENT-ABIETANOS DE Euphorbia phosphorea (EUPHORBIACEAE) by Roseana A. R. Meireles, Lucas S. Abreu, Joanda Paolla R. e Silva, Andreza B. S. Cavalcanti, Renata Priscila B. de Menezes, Gabriela Cristina S. Rodrigues, Valnês S. Rodrigues Junior, José Iranildo M. de Melo, Massuo Jorge Kato, Vicente Carlos de O. Costa, Marcus Tullius Scotti, Josean F. Tavares

“…Phytochemical study of the roots of Euphorbia phosphorea Mart. (Euphorbiaceae) was carried out through chromatographic techniques, resulting in the isolation…”
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Activity of 2-(quinolin-4-yloxy)acetamides in Mycobacterium tuberculosis clinical isolates and identification of their molecular target by whole-genome sequencing by Subtil, Fernanda Teixeira, Villela, Anne Drumond, Abbadi, Bruno Lopes, Rodrigues-Junior, Valnês S., Bizarro, Cristiano Valim, Timmers, Luis Fernando Saraiva Macedo, de Souza, Osmar Norberto, Pissinate, Kenia, Machado, Pablo, López-Gavín, Alexandre, Tudó, Griselda, González-Martín, Julian, Basso, Luiz Augusto, Santos, Diógenes Santiago

“…•Quinoloxyacetamides are active against clinical isolates resistant to main tuberculosis (TB) drugs.•Quinoloxyacetamides do not target DNA gyrase from…”
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Nonclinical evaluation of IQG-607, an anti-tuberculosis candidate with potential use in combination drug therapy by Rodrigues-Junior, Valnês S., Villela, Anne D., Abbadi, Bruno L., Sperotto, Nathalia D.M., Pissinate, Kenia, Picada, Jaqueline N., Bondan da Silva, Juliana, Bizarro, Cristiano V., Machado, Pablo, Basso, Luiz A.

“…New effective compounds to treat tuberculosis are urgently needed. IQG-607 is an orally active anti-tuberculosis drug candidate, with promising preliminary…”
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Effects of tafenoquine against active, dormant and resistant Mycobacterium tuberculosis by Sidrônio, Maria Gabriella S., Castelo Branco, Ana Paula O.T., Abbadi, Bruno L., Macchi, Fernanda, Silveira, Maiele D., Lock, Graziela de A., Costa, Teresa Dalla, de Araújo, Demétrius M., Cibulski, Samuel, Bizarro, Cristiano V., Machado, Pablo, Basso, Luiz Augusto, Rodrigues-Junior, Valnês S.

“…Antimalarial drugs have been suggested as promising scaffolds with anti-tubercular activities. In this work, we demonstrated, for the first time, the…”
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Revisiting Activation of and Mechanism of Resistance to Compound IQG-607 in Mycobacterium tuberculosis by Abbadi, Bruno L, Villela, Anne D, Rodrigues-Junior, Valnês S, Subtil, Fernanda T, Dalberto, Pedro F, Pinheiro, Ana P S, Santos, Diógenes S, Machado, Pablo, Basso, Luiz A, Bizarro, Cristiano V

“…IQG-607 is a metal complex previously reported as a promising anti-tuberculosis (TB) drug against isoniazid (INH)-resistant strains of Unexpectedly, we found…”
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Toxicological profile of IQG-607 after single and repeated oral administration in minipigs: An essential step towards phase I clinical trial by Rodrigues-Junior, Valnês S., Cintra, Luciana, Machado, Pablo, Dadda, Adílio, Basso, Luiz Augusto, Mafra, Ana Carolina Cintra Nunes, Campos, Alexandre Holthausen, Campos, Maria Martha, Santos, Diógenes Santiago

“…IQG-607 is an anti-tuberculosis drug candidate, with a promising safety and efficacy profile in models of tuberculosis infection both in vitro and in vivo…”
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Mefloquine and its oxazolidine derivative compound are active against drug-resistant Mycobacterium tuberculosis strains and in a murine model of tuberculosis infection by Rodrigues-Junior, Valnês S, Villela, Anne D, Gonçalves, Raoni S.B, Abbadi, Bruno Lopes, Trindade, Rogério Valim, López-Gavín, Alexandre, Tudó, Griselda, González-Martín, Julian, Basso, Luiz Augusto, de Souza, Marcus V.N, Campos, Maria Martha, Santos, Diógenes Santiago

“…Highlights • Mefloquine and its oxazolidine derivative 1E were active in a murine model of tuberculosis (TB). • Mefloquine and 1E were active after oral…”
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Preclinical safety evaluation of IQG-607 in rats: Acute and repeated dose toxicity studies by Rodrigues-Junior, Valnês S., Machado, Pablo, Calixto, João B., Siqueira, Jarbas M., Andrade, Edinéia L., Bento, Allisson F., Campos, Maria M., Basso, Luiz A., Santos, Diógenes S.

“…In the present study, we evaluated the safety and the possible toxic effects of IQG-607 after acute and 90-day repeated administrations in rats. Single oral…”
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Preclinical pharmacokinetic profiling of IQG-607, a potential oral metallodrug to treat tuberculosis by Dadda, Adilio da S., Rodrigues-Junior, Valnês S., Carreño, Fernando, Petersen, Guilherme O., Pinto, Antônio F.M., Dalberto, Pedro F., Sperotto, Nathalia D.M., Pissinate, Kenia, Bizarro, Cristiano V., Machado, Pablo, Campos, Maria M., Costa, Teresa Dalla, Santos, Diógenes S., Basso, Luiz A.

“…IQG-607 is an analog of isoniazid with anti-tuberculosis activity. This work describes the development and validation of an HPLC method to quantify…”
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IQG-607 abrogates the synthesis of mycolic acids and displays intracellular activity against Mycobacterium tuberculosis in infected macrophages by Rodrigues-Junior, Valnês S, dos Santos Junior, André A, Villela, Anne D, Belardinelli, Juan M, Morbidoni, Héctor R, Basso, Luiz A, Campos, Maria M, Santos, Diógenes S

“…Abstract In this work, the antitubercular activity of a pentacyano(isoniazid)ferrate(II) compound (IQG-607) was investigated using a macrophage model of…”
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Effect of the bradykinin 1 receptor antagonist SSR240612 after oral administration in Mycobacterium tuberculosis-infected mice by Rodrigues-Junior, Valnês S., Pail, Priscilla B., Villela, Anne D., Falcão, Virgínia C.A., Dadda, Adílio S., Abbadi, Bruno L., Pesquero, João B., Santos, Diógenes S., Basso, Luiz A., Campos, Maria M.

“…The role, if any, played by the kinin system in tuberculosis infection models, either in vivo or in vitro, was investigated. The effects of Mycobacterium…”
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Activity of IQG-607, a new orally active compound, in a murine model of Mycobacterium tuberculosis infection by Rodrigues-Junior, Valnês S, dos Santos Junior, André, dos Santos, Anderson Jader, Schneider, Cristopher Zandoná, Calixto, João B, Sousa, Eduardo Henrique Silva, de França Lopes, Luiz Gonzaga, Souto, André Arigony, Basso, Luiz Augusto, Santos, Diógenes Santiago, Campos, Maria M

“…Abstract We have previously demonstrated a potent in vitro inhibitory activity for two pentacyano(isoniazid)ferrate(II) compounds, namely IQG-607 and IQG-639,…”
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The conserved Lysine69 residue plays a catalytic role in Mycobacterium tuberculosis shikimate dehydrogenase by Rodrigues, Jr, Valnês S, Breda, Ardala, Santos, Diógenes S, Basso, Luiz A

“…The shikimate pathway is an attractive target for the development of antitubercular agents because it is essential in Mycobacterium tuberculosis, the causative…”
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Pre-clinical evaluation of quinoxaline-derived chalcones in tuberculosis by Muradás, Thaís C, Abbadi, Bruno L, Villela, Anne D, Macchi, Fernanda S, Bergo, Pedro F, de Freitas, Talita F, Sperotto, Nathalia D M, Timmers, Luis F S M, Norberto de Souza, Osmar, Picada, Jaqueline N, Fachini, Jean, da Silva, Juliana Bondan, de Albuquerque, Nayara C P, Habenschus, Maísa D, Carrão, Daniel B, Rocha, Bruno A, Barbosa Junior, Fernando, de Oliveira, Anderson R M, Mascarello, Alessandra, Neuenfeldf, Patrícia, Nunes, Ricardo J, Morbidoni, Héctor R, Campos, Maria M, Basso, Luiz A, Rodrigues-Junior, Valnês S

“…New effective compounds for tuberculosis treatment are needed. This study evaluated the effects of a series of quinoxaline-derived chalcones against…”
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