| Id |
Subject |
Object |
Predicate |
Lexical cue |
| T1 |
0-92 |
Sentence |
denotes |
Vipirinin, a coumarin-based HIV-1 Vpr inhibitor, interacts with a hydrophobic region of VPR. |
| T2 |
93-247 |
Sentence |
denotes |
The human immunodeficiency virus 1 (HIV-1) viral protein R (Vpr) is an accessory protein that has been shown to have multiple roles in HIV-1 pathogenesis. |
| T3 |
248-488 |
Sentence |
denotes |
By screening chemical libraries in the RIKEN Natural Products Depository, we identified a 3-phenyl coumarin-based compound that inhibited the cell cycle arrest activity of Vpr in yeast and Vpr-dependent viral infection of human macrophages. |
| T4 |
489-614 |
Sentence |
denotes |
We determined its minimal pharmacophore through a structure-activity relationship study and produced more potent derivatives. |
| T5 |
615-807 |
Sentence |
denotes |
We detected direct binding, and by assaying a panel of Vpr mutants, we found the hydrophobic region about residues Glu-25 and Gln-65 to be potentially involved in the binding of the inhibitor. |
| T6 |
808-983 |
Sentence |
denotes |
Our findings exposed a targeting site on Vpr and delineated a convenient approach to explore other targeting sites on the protein using small molecule inhibitors as bioprobes. |
