2014
DOI: 10.1016/j.bmcl.2014.11.004
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Fragment based search for small molecule inhibitors of HIV-1 Tat-TAR

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Cited by 35 publications
(37 citation statements)
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“…49-52 High-throughput and fragment-based screens have yielded small molecules that bind TAR in the micromolar range and inhibit Tat interactions. 53-57 Recently, small molecule microarrays have been employed by Schneekloth and coworkers to discover a TAR-binding probe that inhibits the HIV-induced cell death of T-lymphocytes at 28 μM without measured toxicity. 17 Importantly, this thienopyridine-based probe was charge neutral and bound TAR with a dissociation constant of 2.4 μM.…”
Section: Introductionmentioning
confidence: 99%
“…49-52 High-throughput and fragment-based screens have yielded small molecules that bind TAR in the micromolar range and inhibit Tat interactions. 53-57 Recently, small molecule microarrays have been employed by Schneekloth and coworkers to discover a TAR-binding probe that inhibits the HIV-induced cell death of T-lymphocytes at 28 μM without measured toxicity. 17 Importantly, this thienopyridine-based probe was charge neutral and bound TAR with a dissociation constant of 2.4 μM.…”
Section: Introductionmentioning
confidence: 99%
“…Their combination led to 2,4,6-triaminoquinazoline (Fig. 7) as the compound with the highest affinity to TAR RNA (IC 50 ¼ 40 μM) [107]. Further investigation of the interaction between 2,4,6-triaminoquinazoline and TAR RNA by 1 H-NMR titrations revealed that this fragment has two distinctive binding sites.…”
Section: Ligands Discovered By Fragment Screening On Rna Targetsmentioning
confidence: 97%
“…Next, we tested the ability of the compounds to displace peptides mimics of the cognate proteins that bind TAR and RREIIB using fluorescence-based assays. These assays have previously been used in screening for an evaluating TAR and RRE binders (Matsumoto et al 2000;Hamasaki and Ueno 2001;Patwardhan et al 2017Patwardhan et al , 2019Zeiger et al 2014). The TAR assay measures fluorescence resonance energy transfer (FRET) of a dual-labeled arginine rich motif (ARM) Tat-mimic peptide (Matsumoto et al 2000;Ganser et al 2018), and the RRE assay measures fluorescence anisotropy of an ARM Rev-mimic peptide (Luedtke and Tor 2003;Chu et al 2019).…”
Section: Assaying Binding Using Rna-peptide Displacement Assaysmentioning
confidence: 99%