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    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.


    Steven E Kirberger, Peter D Ycas, Jorden A Johnson, Chen Chen, Michael F Ciccone, Rinette W L Woo, Andrew K Urick, Huda Zahid, Ke Shi, Hideki Aihara, Sean D McAllister, Mohammed Kashani-Sabet, Junwei Shi, Alex Dickson, Camila O Dos Santos, William C K Pomerantz. Selectivity, ligand deconstruction, and cellular activity analysis of a BPTF bromodomain inhibitor. Organic & biomolecular chemistry. 2019 Feb 13;17(7):2020-2027

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    PMID: 30706071

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