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| Solution Information | help | |
| Enzyme: | PC4 and SFRS1-interacting protein | |
| inhibitor: | BDBM54904 | |
| substrate: | n/a | |
| Solution Type: | Aqueous | |
| pH at Preparation: | n/a | |
| Temp. Prep.: | n/a | |
| Comments: | Assay Overview: The purpose of this biochemical assay is to determine dose response curves for compounds that confirm inbitory activity a set of previous experimetns entitled: "Confirmation assay for inhibitors of LEDGF/p75-dependent integration: TR-FRET-based biochemical high throughput assay to identify inhibitors of HIV-1 LEDGF/p75 DNA Integration." (AID 1053136). The main novelty of our approach is to discover new probes that stabilize functionally compromised IN multimers rather than interfere with IN multimerization. Here we refer to such probes as MINIs (multimeric IN inhibitors). Discovery of MINIs through HTS will provide a new and powerful tool for structural and mechanistic studies to elucidate how different multimeric forms of IN interact with viral DNA as well as viral and cellular proteins at different stages of viral replication. In this assay, test compounds are incubated with IN, followed by addition of DNA Substrates (50nM viral DNA-Cy5, 10nM target DNA substrate f | |
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