26819-11-4Relevant academic research and scientific papers
Selectivity, ligand deconstruction, and cellular activity analysis of a BPTF bromodomain inhibitor
Kirberger, Steven E.,Ycas, Peter D.,Johnson, Jorden A.,Chen, Chen,Ciccone, Michael F.,Woo, Rinette W. L.,Urick, Andrew K.,Zahid, Huda,Shi, Ke,Aihara, Hideki,McAllister, Sean D.,Kashani-Sabet, Mohammed,Shi, Junwei,Dickson, Alex,Dos Santos, Camila O.,Pomerantz, William C. K.
supporting information, p. 2020 - 2027 (2019/02/20)
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.
11a-Methano-TXA compounds
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, (2008/06/13)
The present invention provides novel 11a-methano-TXA compounds and intermediates and processs for their preparation. Further provided are methods for using these novel TXA analogs as inhibitors of thromboxane synthetase, rendering these analogs useful for a variety of pharmacological purposes. These pharmacological uses include anti-inflammatory, anti-thromobitc, and anti-asthma indications.
