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Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Usi

Journal Article · · J. Med. Chem.
Research Organization:
Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
Sponsoring Organization:
DOE - Office Of Science; INDUSTRY
OSTI ID:
1834907
Journal Information:
J. Med. Chem., Journal Name: J. Med. Chem. Journal Issue: (19) Vol. 64
Country of Publication:
United States
Language:
ENGLISH

References (31)

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Bromodomain: an acetyl-lysine binding domain journal January 2002
Integration, scaling, space-group assignment and post-refinement journal January 2010
Achieving clinical success with BET inhibitors as anti-cancer agents journal March 2021
Syntheses and Binding Studies of New [(Aryl)(aryloxy)methyl]piperidine Derivatives and Related Compounds as Potential Antidepressant Drugs with High Affinity for Serotonin (5-HT) and Norepinephrine (NE) Transporters journal November 2003
Scaling and assessment of data quality journal December 2005
Structural Modifications that Alter the P-Glycoprotein Efflux Properties of Compounds journal April 2012
Phaser crystallographic software journal July 2007
Interplay between epigenetics and metabolism in oncogenesis: mechanisms and therapeutic approaches journal January 2017
Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers journal April 2013
Protein and ligand preparation: parameters, protocols, and influence on virtual screening enrichments journal March 2013
BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells journal May 2015
Progress in the Development and Application of Small Molecule Inhibitors of Bromodomain–Acetyl-lysine Interactions journal September 2012
Functions of Site-Specific Histone Acetylation and Deacetylation journal June 2007
RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia journal August 2011
Suppression of inflammation by a synthetic histone mimic journal November 2010
Refinement of severely incomplete structures with maximum likelihood in BUSTER–TNT journal November 2004
Inhibition of BET Bromodomain Targets Genetically Diverse Glioblastoma journal February 2013
Targeting MYC dependence in cancer by inhibiting BET bromodomains journal September 2011
Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer. journal November 2013
Efficacy of BET Bromodomain Inhibition in Kras-Mutant Non–Small Cell Lung Cancer journal September 2013
BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc journal September 2011
Sensitivity of Small Cell Lung Cancer to BET Inhibition Is Mediated by Regulation of ASCL1 Gene Expression journal August 2015
Beamline 08ID-1, the prime beamline of the Canadian Macromolecular Crystallography Facility journal June 2011
Abstract 5789: Discovery of clinical candidate BMS-986158, an oral BET inhibitor, for the treatment of cancer conference July 2018
Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia journal October 2011
Selective inhibition of BET bromodomains journal September 2010
BET inhibitor resistance emerges from leukaemia stem cells journal September 2015
The bromodomain interaction module journal May 2012

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