Ontology highlight
ABSTRACT:
SUBMITTER: Kirberger SE
PROVIDER: S-EPMC6374164 | biostudies-literature | 2019 Feb
REPOSITORIES: biostudies-literature
Kirberger Steven E SE Ycas Peter D PD Johnson Jorden A JA Chen Chen C Ciccone Michael F MF Woo Rinette W L RWL Urick Andrew K AK Zahid Huda H Shi Ke K Aihara Hideki H McAllister Sean D SD Kashani-Sabet Mohammed M Shi Junwei J Dickson Alex A Dos Santos Camila O CO Pomerantz William C K WCK
Organic & biomolecular chemistry 20190201 7
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 ana ...[more]