Small molecule inhibitors of HIV RT Ribonuclease H.
Di Grandi M, Olson M, Prashad AS, Bebernitz G, Luckay A, Mullen S, Hu Y, Krishnamurthy G, Pitts K, O'Connell J
Bioorganic & medicinal chemistry letters (2010), Volume 20, Page 398
Abstract:
Two classes of compounds, thiocarbamates 1 and triazoles 2, have been identified as HIV RT RNase H inhibitors using a novel FRET-based HTS assay. The potent analogs in each series exhibited selectivity and were active in cell-based assays. In addition, saturable, 1:1 stoichiometric binding to target was established and time of addition studies were consistent with inhibition of RT-mediated HIV replication.
Polymerases:
Topics:
Modulators/Inhibitors, Health/Disease, RNase H Activity
Status:
| new | topics/pols set | partial results | complete | validated |
Results:
No results available for this paper.