Mechanism of Inhibition of HIV-1 Reverse Transcriptase by the Novel Broad-range DNA Polymerase Inhibitor N-{2-[4-(aminosulfonyl)phenyl]ethyl}-2-(2-thienyl)acetamide

Employing a novel strategy, we have virtually screened a large library of compounds to identify novel inhibitors of the reverse transcriptase (RT) of HIV-1. Fifty-six top scored compounds were tested in vitro, and two of them inhibited efficiently the DNA polymerase activity of RT. The most effective compound, N-{2-[4-(aminosulfonyl)phenyl]ethyl}-2-(2-thienyl)acetamide (NAPETA), inhibited both RNA-dependent and DNA-dependent … Continued

Transfer-NMR and Docking Studies Identify the Binding of the Peptide Derived from Activating Transcription Factor 4 to Protein Ubiquitin Ligase Beta-TrCP; Competition STD-NMR with β-catenin

ATF4 plays a crucial role in the cellular response to stress. The E3 ubiquitin ligase, SCF β-TrCP protein responsible for ATF4 degradation by the proteasome, binds to ATF4 through a DpSGXXXpS phosphorylation motif, which is similar but not identical to the DpSGXXpS motif found in most other substrates of β-TrCP. NMR studies were performed on … Continued

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