Skip to main content
U.S. Department of Energy
Office of Scientific and Technical Information

RETURN TO ISSUEPREVARTICLENEXT New Design Rules for Developing Potent Cell-Active Inhibitors of the

Journal Article · · J. Med. Chem.

Research Organization:
Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
Sponsoring Organization:
DOE - Office Of Science; NIH
OSTI ID:
1825752
Journal Information:
J. Med. Chem., Journal Name: J. Med. Chem. Journal Issue: (18) Vol. 64
Country of Publication:
United States
Language:
ENGLISH

References (48)

Cell permeability beyond the rule of 5 journal June 2016
Recognition of a Mononucleosomal Histone Modification Pattern by BPTF via Multivalent Interactions journal May 2011
BPTF promotes tumor growth and predicts poor prognosis in lung adenocarcinomas journal September 2015
Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family journal March 2012
The molecular hallmarks of epigenetic control journal June 2016
Epigenetics: A Landscape Takes Shape journal February 2007
A rationale to target the SWI/SNF complex for cancer therapy journal August 2014
BPTF Maintains Chromatin Accessibility and the Self-Renewal Capacity of Mammary Gland Stem Cells journal July 2017
Features and development of Coot journal March 2010
Essential Role of Chromatin Remodeling Protein Bptf in Early Mouse Embryos and Embryonic Stem Cells journal October 2008
Isolation of human NURF: a regulator of Engrailed gene expression journal November 2003
PHENIX: a comprehensive Python-based system for macromolecular structure solution journal January 2010
BPTF, a chromatin remodeling-related gene, exhibits frameshift mutations in gastric and colorectal cancers journal February 2016
Fluorinated Aromatic Amino Acids Are Sensitive 19 F NMR Probes for Bromodomain-Ligand Interactions journal October 2014
Selectivity, ligand deconstruction, and cellular activity analysis of a BPTF bromodomain inhibitor journal January 2019
Sustained activation of STAT5 is essential for chromatin remodeling and maintenance of mammary-specific function journal January 2009
Druggability Analysis and Structural Classification of Bromodomain Acetyl-lysine Binding Sites journal July 2012
Mammalian SWI/SNF complexes in cancer: emerging therapeutic opportunities journal February 2017
BPTF promotes hepatocellular carcinoma growth by modulating hTERT signaling and cancer stem cell traits journal January 2019
The role of ligand efficiency metrics in drug discovery journal January 2014
Selective N‐Terminal BET Bromodomain Inhibitors by Targeting Non‐Conserved Residues and Structured Water Displacement** journal November 2020
The Role of BPTF in Melanoma Progression and in Response to BRAF-Targeted Therapy journal February 2015
BPTF regulates growth of adult and pediatric high-grade glioma through the MYC pathway journal December 2019
Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains journal May 2020
Dual Screening of BPTF and Brd4 Using Protein-Observed Fluorine NMR Uncovers New Bromodomain Probe Molecules journal July 2015
Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel–Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7 journal December 2018
Synthesis of NVS-BPTF-1 and evaluation of its biological activity journal September 2021
New inhibitors for the BPTF bromodomain enabled by structural biology and biophysical assay development journal January 2020
Bromodomain PHD‑finger transcription factor promotes glioma progression and indicates poor prognosis journal October 2018
Autophagy-Dependent Sensitization of Triple-Negative Breast Cancer Models to Topoisomerase II Poisons by Inhibition of the Nucleosome Remodeling Factor journal April 2021
c-MYC partners with BPTF in human cancer journal May 2016
Chromatin-Remodelling Complex NURF Is Essential for Differentiation of Adult Melanocyte Stem Cells journal October 2015
Opportunity knocks for uncovering the new function of an understudied nucleosome remodeling complex member, the bromodomain PHD finger transcription factor, BPTF journal August 2021
Off-target toxicity is a common mechanism of action of cancer drugs undergoing clinical trials journal September 2019
Mechanisms of action and regulation of ATP-dependent chromatin-remodelling complexes journal May 2017
BPTF Is Essential for T Cell Homeostasis and Function journal October 2016
Discovery of selective BPTF bromodomain inhibitors by screening and structure-based optimization journal March 2021
Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe journal January 2017
BPTF Depletion Enhances T-cell–Mediated Antitumor Immunity journal September 2016
XDS journal January 2010
Advancements in the Development of non‐BET Bromodomain Chemical Probes journal January 2019
BPTF is required for c-MYC transcriptional activity and in vivo tumorigenesis journal January 2016
Dual Functions of Largest NURF Subunit NURF301 in Nucleosome Sliding and Transcription Factor Interactions journal September 2001
Identification and Characterization of BPTF, a Novel Bromodomain Transcription Factor journal January 2000
Domain-selective targeting of BET proteins in cancer and immunological diseases journal August 2020
Differentiation of Mouse Breast Epithelial HC11 and EpH4 Cells journal January 2020
BET domain co-regulators in obesity, inflammation and cancer journal June 2012
Systematically Mitigating the p38α Activity of Triazole-based BET Inhibitors journal August 2019

Similar Records

New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (N
Journal Article · 2021 · J. Med. Chem. · OSTI ID:1828955

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells
Journal Article · 2015 · Proc. Natl. Acad. Sci. USA · OSTI ID:1164191

Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase
Journal Article · 2022 · Bioorganic and Medicinal Chemistry Letters · OSTI ID:1981547

Related Subjects