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• W2914035046 endingPage "2027" @default.
• W2914035046 startingPage "2020" @default.
• W2914035046 abstract "Bromodomain and PHD finger containing protein transcription factor (BPTF) is an epigenetic protein involved in chromatin remodelling and is a potential anticancer target. The BPTF bromodomain has one reported small molecule inhibitor (AU1, rac-1). Here, advances made on the structure-activity relationship of a BPTF bromodomain ligand are reported using a combination of experimental and molecular dynamics simulations leading to the active enatiomer (S)-1. Additionally, a ligand deconstruction analysis was conducted to characterize important pharmacophores for engaging the BPTF bromodomain. These studies have been enabled by a protein-based fluorine NMR approach, highlighting the versatility of the method for selectivity, ligand deconstruction, and ligand binding. To enable future analysis of biological activity, cell growth analyses in a panel of cancer cell lines were carried out using CRISPR-Cas9 and (S)-1 to identify cell-based model systems that are sensitive to BPTF inhibition." @default.
• W2914035046 created "2019-02-21" @default.
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• W2914035046 date "2019-01-01" @default.
• W2914035046 modified "2023-10-16" @default.
• W2914035046 title "Selectivity, ligand deconstruction, and cellular activity analysis of a BPTF bromodomain inhibitor" @default.
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• W2914035046 doi "https://doi.org/10.1039/c8ob02599a" @default.
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• W2914035046 hasPublicationYear "2019" @default.
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