Screening For Small Molecule Inhibitors Of HIV-1 VPR: Discovery Of Vipirinin And Its Use As A Bioprobe
The human immunodeficiency virus 1 (HIV-1) viral protein R (Vpr) is an accessory protein that has been known to have multiple roles in HIV-1 pathogenesis. Here, a high-throughput screening (HTS) system was developed to screen chemical libraries in RIKEN Natural Products Depository (NPDepo). Through...
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| Format: | Thesis |
| Language: | English |
| Published: |
2011
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| Subjects: | |
| Online Access: | http://eprints.usm.my/41785/1/EUGENE_ONG_BOON_BENG.pdf http://eprints.usm.my/41785/ |
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| Summary: | The human immunodeficiency virus 1 (HIV-1) viral protein R (Vpr) is an accessory protein that has been known to have multiple roles in HIV-1 pathogenesis. Here, a high-throughput screening (HTS) system was developed to screen chemical libraries in RIKEN Natural Products Depository (NPDepo). Through HTS, NPD4456, a 3-phenyl coumarin based compound, was identified to be an inhibitor of the cell cycle arrest activity of Vpr in yeast. The minimal pharmacophore of the inhibitor was determined through a structure-activity relationship study and more potent derivatives were produced. |
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