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3 results on '"allnis"'

1. The selenium-containing drug ebselen potently disrupts LEDGF/p75-HIV-1 integrase interaction by targeting LEDGF/p75

Author

Da-Wei Zhang, Hao-Li Yan, Xiao-Shuang Xu, Lei Xu, Zhi-Hui Yin, Shan Chang, and Heng Luo

Subjects
allnis, integrase, ledgf/p75-integrase interaction, hiv-1, Therapeutics. Pharmacology, RM1-950
Abstract

Lens-epithelium-derived growth-factor (LEDGF/p75)-binding site on HIV-1 integrase (IN), is an attractive target for antiviral chemotherapy. Small-molecule compounds binding to this site are referred as LEDGF-IN inhibitors (LEDGINs). In this study, compound libraries were screened to identify new inhibitors of LEDGF/p75-IN interaction. Ebselen (2-phenyl-1,2-benzisoselenazol-3-one), a reported anti-HIV-1 agent, was identified as a moderate micromolar inhibitor of LEDGF/p75-IN interaction. Ebselen inhibited the interaction by binding to LEDGF/p75 and the ability of ebselen to inhibit the interaction could be reversed by dithiothreitol (DTT). BLI experiment showed that ebselen probably formed selenium-sulphur bonds with reduced thiols in LEDGF/p75. To the best of our knowledge, we showed for the first time that small-molecule compound, ebselen inhibited LEDGF/p75-IN interaction by directly binding to LEDGF/p75. The compound discovered here could be used as probe compounds to design and develop new disrupter of LEDGF/p75-IN interaction.

Published
2020
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2. The selenium-containing drug ebselen potently disrupts LEDGF/p75-HIV-1 integrase interaction by targeting LEDGF/p75.

Author

Zhang, Da-Wei, Yan, Hao-Li, Xu, Xiao-Shuang, Xu, Lei, Yin, Zhi-Hui, Chang, Shan, and Luo, Heng

Subjects
BINDING sites, THIOLS, RALTEGRAVIR, DRUGS, CANCER chemotherapy, EBSELEN
Abstract

Lens-epithelium-derived growth-factor (LEDGF/p75)-binding site on HIV-1 integrase (IN), is an attractive target for antiviral chemotherapy. Small-molecule compounds binding to this site are referred as LEDGF-IN inhibitors (LEDGINs). In this study, compound libraries were screened to identify new inhibitors of LEDGF/p75-IN interaction. Ebselen (2-phenyl-1,2-benzisoselenazol-3-one), a reported anti-HIV-1 agent, was identified as a moderate micromolar inhibitor of LEDGF/p75-IN interaction. Ebselen inhibited the interaction by binding to LEDGF/p75 and the ability of ebselen to inhibit the interaction could be reversed by dithiothreitol (DTT). BLI experiment showed that ebselen probably formed selenium-sulphur bonds with reduced thiols in LEDGF/p75. To the best of our knowledge, we showed for the first time that small-molecule compound, ebselen inhibited LEDGF/p75-IN interaction by directly binding to LEDGF/p75. The compound discovered here could be used as probe compounds to design and develop new disrupter of LEDGF/p75-IN interaction. [ABSTRACT FROM AUTHOR]

Published
2020
Full Text
View/download PDF

3. The selenium-containing drug ebselen potently disrupts LEDGF/p75-HIV-1 integrase interaction by targeting LEDGF/p75

Author

Hao-Li Yan, Heng Luo, Zhi-Hui Yin, Da-Wei Zhang, Xu Xiaoshuang, Lei Xu, and Shan Chang

Subjects
Drug, Azoles, musculoskeletal diseases, Antiviral chemotherapy, Anti-HIV Agents, media_common.quotation_subject, ledgf/p75-integrase interaction, Drug Evaluation, Preclinical, chemistry.chemical_element, hiv-1, HIV Integrase, Microbial Sensitivity Tests, RM1-950, Pharmacology, Isoindoles, 01 natural sciences, Dithiothreitol, chemistry.chemical_compound, Structure-Activity Relationship, Organoselenium Compounds, Drug Discovery, Humans, HIV Integrase Inhibitors, media_common, Binding Sites, allnis, biology, Dose-Response Relationship, Drug, Molecular Structure, 010405 organic chemistry, Ebselen, General Medicine, biological factors, 0104 chemical sciences, Integrase, 010404 medicinal & biomolecular chemistry, chemistry, nervous system, Hiv 1 integrase, biology.protein, Intercellular Signaling Peptides and Proteins, sense organs, integrase, Therapeutics. Pharmacology, Selenium, Research Paper
Abstract

Lens-epithelium-derived growth-factor (LEDGF/p75)-binding site on HIV-1 integrase (IN), is an attractive target for antiviral chemotherapy. Small-molecule compounds binding to this site are referred as LEDGF-IN inhibitors (LEDGINs). In this study, compound libraries were screened to identify new inhibitors of LEDGF/p75-IN interaction. Ebselen (2-phenyl-1,2-benzisoselenazol-3-one), a reported anti-HIV-1 agent, was identified as a moderate micromolar inhibitor of LEDGF/p75-IN interaction. Ebselen inhibited the interaction by binding to LEDGF/p75 and the ability of ebselen to inhibit the interaction could be reversed by dithiothreitol (DTT). BLI experiment showed that ebselen probably formed selenium-sulphur bonds with reduced thiols in LEDGF/p75. To the best of our knowledge, we showed for the first time that small-molecule compound, ebselen inhibited LEDGF/p75-IN interaction by directly binding to LEDGF/p75. The compound discovered here could be used as probe compounds to design and develop new disrupter of LEDGF/p75-IN interaction.

Published
2020

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