Cyp51
Mostrando 1-12 de 73 artigos, teses e dissertações.
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1. Tandem Synthesis of Furanaphthoquinones via Enamines and Evaluation of Their Antiparasitic Effects against Trypanosoma cruzi
Furanaphthoquinones are well known in medicinal chemistry for exhibiting relevant structural heterogeneity and bioactivities. In this work, it was synthesized a series of furanaphthoquinones through a tandem reaction between lawsone (8) and cyclic ketones in the presence of morpholine. This strategy provides an efficient and general method for synthesizing f
Journal of the Brazilian Chemical Society. Publicado em: 2022
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2. CYP450 Metabolism of a Semisynthetic Naphthoquinone, an Anticancer Drug Candidate, by Human Liver Microsomes
CNFD (6b,7-dihydro-5H-cyclopenta[b]naphtho[2,1-d]furan-5,6(9aH)-dione) is a semisynthetic naphthoquinone derived from lawsone that has cytotoxic action in different tumor lines and anticancer activity in vivo. Therefore, this molecule is a relevant candidate for drug development, but there is still no information on its human metabolism and systemic eliminat
Journal of the Brazilian Chemical Society. Publicado em: 2022
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3. Resistance to triazole fungicides in Pyricularia species is associated with invasive plants from wheat fields in Brazil
ABSTRACT. Triazole fungicides have not been effective for managing the wheat blast disease in Brazil. A broad analysis across six geographical populations of Pyricularia graminis-tritici in central-southern Brazil indicated a high level of resistance to triazole fungicides. Since P. graminis-tritici is also associated with others poaceous species, here, we a
Acta Sci., Agron.. Publicado em: 13/06/2019
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4. Novel point mutations in the ERG11 gene in clinical isolates of azole resistant Candida species
The azoles are the class of medications most commonly used to fight infections caused by Candida sp. Typically, resistance can be attributed to mutations in ERG11 gene (CYP51) which encodes the cytochrome P450 14α-demethylase, the primary target for the activity of azoles. The objective of this study was to identify mutations in the coding region of theERG1
Mem. Inst. Oswaldo Cruz. Publicado em: 15/03/2016
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5. CYP3A5 genotyping for assessing the efficacy of treatment with simvastatin and atorvastatin
In this work, we examined the impact of polymorphism in the cytochrome P450 (CYP) 3A5 gene, CYP3A5*1 (6986A > G, rs 776746), on the reduction in the lipid levels caused by simvastatin and atorvastatin. We studied 350 hyperlipidemic patients who received 10-40 mg of atorvastatin (n = 175) or simvastatin (n = 175) daily. Genotyping for CYP3A5 was done by PCR-R
Genet. Mol. Biol.. Publicado em: 2015-06
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6. Hologram- and descriptor-based QSAR studies for a series of non-azoles derivatives active against C. neoformans
Durante as últimas décadas as infecções fúngicas têm se tornado um crescente problema de saúde, especialmente para pacientes imunocomprometidos. Infelizmente, o padrão-ouro de terapia profilática para tal doença é baseada em derivados azólicos, que são mais fungistáticos do que fungicidas contra C. neoformans e causam hepatotoxicidade. Objetiva
J. Braz. Chem. Soc.. Publicado em: 2013-10
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7. The stepwise selection for ketoconazole resistance induces upregulation of C14-demethylase (CYP51) in Leishmania amazonensis
Ketoconazole is a clinically safe antifungal agent that also inhibits the growth of Leishmania spp. A study was undertaken to determine whether Leishmania parasites are prone to becoming resistant to ketoconazole by upregulating C14-demethylase after stepwise pharmacological pressure. Leishmania amazonensis promastigotes [inhibitory concentration (IC)50 = 2
Memórias do Instituto Oswaldo Cruz. Publicado em: 2012-05
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8. Influência da variabilidade genética sobre biomarcadores de dano oxidativo e não oxidativo em pacientes com doença pulmonar obstrutiva crônica (DPOC)
Chronic Obstructive Pulmonary Disease (COPD) is a slowly progressive condition of poor reversibility that is characterized by airflow limitation associated with an abnormal inflammatory response of the lungs. Its development and progression are related to increased oxidative stress, which is an important pathogenic component of airway inflammation in this di
IBICT - Instituto Brasileiro de Informação em Ciência e Tecnologia. Publicado em: 2012
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9. Efeitos de hipolipemiantes sobre a expressão de CYP3A4 e CYP3A5 in vitro e in vivo / Hypolipemiant effects on CYP3A4 and CYP3A5 mRNA expression in vitro and in vivo
Introdução: As CYP3A4 e CYP3A5 são enzimas do citocromo P450 responsáveis pela biotransformação de esteróides endógenos e vários fármacos, entre eles as estatinas. Polimorfismos nos genes CYP3A4 e CYP3A5 (CYP3A4*1B, CYP3A5*3C e CYP3A5*1D) foram associados com diferenças na resposta hipolipemiante de indivíduos tratados com atorvastatina e sinvast
IBICT - Instituto Brasileiro de Informação em Ciência e Tecnologia. Publicado em: 07/10/2011
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10. Farmacocinética e PK-PD dos isômeros do nebivolol em voluntários sadios metabolizadores extensivos ou lentos para o CYP2D6 / Pharmacokinetics and PK-PD of the isomers of nebivolol in healthy volunteers extensive metabolisers or poor metabolisers for CYP2D6.
O nebivolol, um fármaco com quatro centros quirais, está disponível na clínica como mistura racêmica dos isômeros d-nebivolol (SRRR) e l-nebivolol (RSSS). A atividade -adrenérgica do nebivolol reside no isômero d-nebivolol, enquanto o l-nebivolol promove a liberação de óxido nítrico das células endoteliais. O nebivolol é eliminado por metabolis
IBICT - Instituto Brasileiro de Informação em Ciência e Tecnologia. Publicado em: 31/08/2011
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11. Mutational analysis of xenobiotic metabolizing genes (CYP1A1 and GSTP1) in sporadic head and neck cancer patients
CYP1A1 is the phase I enzyme that detoxifies the carcinogen or converts it into a more electrophilic form, metabolized by phase II enzymes like GSTP1. These detoxifying genes have been extensively studied in association with head and neck cancer (HNC) in different ethnic groups worldwide. The current study was aimed at screening genetic polymorphisms of gene
Genetics and Molecular Biology. Publicado em: 19/08/2011
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12. Risco ocupacional em fumicultores : genotoxicidade associada à suscetibilidade genética
Agricultores envolvidos no cultivo do tabaco estão constantemente expostos a uma grande variedade de químicos. O uso de agrotóxicos em larga escala tem provocado danos à saúde destes trabalhadores assim como a manipulação das folhas de fumo úmidas, pois além de substâncias antropogênicas persistentes outros compostos orgânicos com potencial pesti
IBICT - Instituto Brasileiro de Informação em Ciência e Tecnologia. Publicado em: 2011