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Identification of arylamine n-acetyltransferase inhibitors as an approach towards novel anti-tuberculars

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Protein & Cell 2010年第1期1卷 82-95页

作者： Isaac M.Westwood Sanjib Bhakta Angela J.Russell Elizabeth Fullam Matthew C.Anderton Akane Kawamura Andrew W.Mulvaney Richard J.Vickers Veemal Bhowruth Gurdyal S.Besra Ajit Lalvani Stephen G.Davies Edith Sim Department of Pharmacology University of OxfordOxford OX13QTUnited Kingdom Chemistry Research Laboratory Department of Organic ChemistryUniversity of OxfordOxford OX13QLUnited Kingdom School of Biosciences University of BirminghamEdgbastonBirmingham B152TTUnited Kingdom Tuberculosis Immunology Group Department of Respiratory MedicineNational Heart and Lung InstituteWright Fleming Institute of Infection and ImmunityImperial College LondonNorfolk PlaceLondon W21PGUnited Kingdom Structure-Based Drug Design Team Sections of Structural Biology and Cancer TherapeuticsInstitute of Cancer ResearchChester Beatty LaboratoriesLondon SW36JBUnited Kingdom Institute of Structural and Molecular Biology Department of Biological ScienceBirkbeckUniversity of LondonLondon WC1E 7HXUnited Kingdom

new anti-tubercular drugs and drug targets are urgently needed to reduce the time for treatment and also to identify agents that will be effective against Mycobacterium tuberculosis persisting *** have a unique cell *** of the gene for arylamine n-acetyltransferase(nAT)decreases mycobacterial cell wall lipids,particularly the distinctive mycolates,and also increases antibiotic susceptibility and killing within macrophage of Mycobacterium bovis *** nat gene and its associated gene cluster are almost identical in sequence in *** BCG and *** gene cluster is essential for intracellular survival of *** have therefore used pure nAT protein for high-throughput screening to identify several classes of small molecules that inhibit nAT ***,we characterize one class of such molecules—triazoles—in relation to its effects on the target enzyme and on both *** BCG and *** most potent triazole mimics the effects of deletion of the nat gene on growth,lipid disruption and intracellular *** also present the structure-activity relationship between nAT inhibition and effects on mycobacterial growth,and use ligand-protein analysis to give further insight into the structure-activity *** conclude that screening a chemical library with nAT protein yields compounds that have high potential as anti-tubercular agents and that the inhibitors will allow further exploration of the biochemical pathway in which nAT is involved.

关键词： n-acetyltransferase Mycobacterium tuberculosis triazoles screening

n-acetyltransferase 2: Slow, intermediate or fast? A booming question of the molecular epidemiology in cancer research

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Open Journal of Genetics 2012年第4期2卷 221-235页

作者： Giuliano Di Pietro Sandra Rocha Gadelha Sandra Mara Bispo Sousa Paulo Roberto Santana de Melo Fabricio Rios Santos Federal University of Mato Grosso Cuiaba Brazil Federal University of Sergipe Lagarto Brazil State University of Santa Cruz Ilhéus Brazil State University of Southwest Bahia Vitória da Conquista Brazil

Throughout history, humanity has referred to reactions occurring with food, plants and, recently, medicines or drugs. The increase in pulmonary tuberculosis cases and the availability of treatment showed that genetic human differences can interfere in the capacity to metabolize drugs. There are remarkable genetic polymorphisms of n-acetyltransferase 2 (nAT2) activity that have been associated with different levels of susceptibility to developing many kinds of cancers. This review considers the field as an open window for the application of molecular epidemiology tools that led to the development of pharmacogenomics. We cover historical data and the most recent knowledge about nAT2 genetic polymorphisms and its distribution in different populations, which is an important concept being incorporated in epidemiological studies of cancer risk. We present up to date information about these studies, including meta-analysis based on the nAT2 distribution in different types of cancer. A critical broad at advances in nAT2 research, high-lighting recent studies related to nAT2 alleles in cancer susceptibility. Although there are multifactorial aspects involved in cancer risk, the variability in nAT2 allelic frequency can be related to carcinogenesis through alterations in the metabolic rate after exposure to carcinogens.

关键词： Cancer Ethnicity Genetic Variants n-acetyltransferase 2

Cloning, Expression and Functional Study of n-acetyltransferase from Bombyx mori

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Cloning, Expression and Functional Study of N-acetyltransfer...

Isoniazid metabolism and hepatotoxicity

中国生物化学与分子生物学会2016年全国学术会议

作者： Huaixiang Zhou Xusheng Cheng Tong Zhang Zuoming nie Qing Sheng College of Life Sciences Zhejiang Sci-Tech University Zhejiang Provincial Key Laboratory of Silkworm Bioreactor and Biomedicine

n-acetyltransferase(nAT)is a kind of enzyme that catalyzes the transfer of acetyl group between acetyl-co A and *** mori,a model lepidoptera insect,is an economic *** this study,according to Bombyx mori nAT gene(Bm nA... 详细信息

关键词： n-acetyltransferase expression profile subcellular localization Immunoprecipitation

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Acta Pharmaceutica Sinica B 2016年第5期6卷 384-392页

作者： Pengcheng Wang Komal Pradhan Xiao-bo Zhong Xiaochao Ma Center for Pharmacogenetics Department of Pharmaceutical SciencesSchool of PharmacyUniversity of Pittsburgh Department of Pharmaceutical Sciences School of PharmacyUniversity of Connecticut

Isoniazid(InH) is highly effective for the management of ***,it can cause liver injury and even liver *** metabolism has been thought to be associated with InH-induced liver *** review summarized the metabolic pathway... 详细信息

关键词： Isoniazid Metabolism Hepatotoxicity Anti-tuberculosis n-acetyltransferase 2 Amidase

Molecular Docking and ADMET Study of Emodin Derivatives as Anticancer Inhibitors of nAT2, COX2 and TOP1 Enzymes

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Computational Molecular Bioscience 2017年第1期7卷 1-18页

作者： Daniel M. Shadrack Valence M. K. ndesendo Chemistry Department Faculty of Natural and Applied Sciences St. John’s University of Tanzania Dodoma Tanzania Department of Pharmaceutics and Formulation Sciences School of Pharmacy and Pharmaceutical Sciences St. John’s University of Tanzania Dodoma Tanzania

Over the past years natural products and/or their derivatives have continued to provide cancer chemotherapeutics. Glycosides derivatives of emodin are known to possess anticancer activities. An in silico study was carried out to evaluate emodin derivatives as inhibitors of Arylamine n-acetyltransferase 2, Cyclooxygenase 2 and Topoisomerase 1 enzymes, predict their pharmacokinetics and explore their bonding modes. Molecular docking study suggested that D2, D5, D6 and D9 to be potent inhibitors of nAT2, while D8 was suggested to be a potent inhibitor of TOP1. Derivatives D2, D5, D6 and D9 bind to the same pocket with different binding conformation. Pharmacokinetic study suggested that selected emodin derivatives can be potential cancer chemotherapeutic agent. Physicochemical parameters such density, balaban index, surface tension, logP and molar reflectance correlated to compounds activity. These finding provides a potential strategy towards developing nAT2 and TOP1 inhibitors.

关键词： Human Arylamine n-acetyltransferase 2 (nAT2) Cyclooxygenase 2 (COX2) Topoisomerase 1 (TOP1) Emodin In Silico Inhibition Pharmacokinetics Molecular Docking

Trimethoprim-Sulfamethoxazole-Induced Hepatitis in Mixed Connective Tissue Disease

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International Journal of Clinical Medicine 2011年第5期2卷 629-632页

作者： Takeshi Sugimoto Yumiko nobuhara Seiji Kawano Akio Morinobu 不详

Trimethoprim-Sulfamethoxazole (TMP-SMZ) is associated with severe hepatic toxicity or liver failure. We present a case of severe hepatic toxicity for whom TMP-SMZ was prescribed as part of treatment for mixed connective tissue disease (MCTD). TMP-SMZ was used to prevent complications from steroid therapy, but fever and hepatic toxicity developed with repeated TMP-SMZ medication. While the drug lymphocyte stimulation test (DLST) for TMP-SMZ showed negative, the genotype for n-acetyltransferase 2 (nAT2) showed type *6/*7, which is the slow acetylating type for nAT2 activity. This finding for nAT2 genotype and the patient’s clinical history lead us to speculate that her fever and hepatic toxicity were caused by TMP-SMZ.

关键词： Hepatic toxicity Mixed Connective Tissue Disease n-acetyltransferase 2 Trimethoprim-Sulfamethoxazole