brahma: A regulator of Drosophila homeotic genes structurally related to the yeast transcriptional activator SNF2SWI2
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February 1992 |
Structure and ligand of a histone acetyltransferase bromodomain
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June 1999 |
Readout of Epigenetic Modifications
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June 2013 |
BET domain co-regulators in obesity, inflammation and cancer
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June 2012 |
Epigenetic protein families: a new frontier for drug discovery
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April 2012 |
Inhibition of bromodomain and extra-terminal proteins (BET) as a potential therapeutic approach in haematological malignancies: emerging preclinical and clinical evidence
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February 2015 |
Bromodomain and extra-terminal domain bromodomain inhibition prevents synovial inflammation via blocking IκB kinase–dependent NF-κB activation in rheumatoid fibroblast-like synoviocytes
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August 2015 |
BET bromodomain inhibition as a novel strategy for reactivation of HIV-1
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December 2012 |
The BET-Bromodomain Inhibitor JQ1 Reduces Inflammation and Tau Phosphorylation at Ser396 in the Brain of the 3xTg Model of Alzheimer's Disease
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July 2016 |
Small-Molecule Inhibition of BRDT for Male Contraception
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August 2012 |
Selective inhibition of BET bromodomains
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September 2010 |
Suppression of inflammation by a synthetic histone mimic
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November 2010 |
Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia
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October 2011 |
Targeting bromodomains: epigenetic readers of lysine acetylation
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April 2014 |
Discovery and Characterization of Small Molecule Inhibitors of the BET Family Bromodomains
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June 2011 |
Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors
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July 2013 |
Structure-Guided Design of Potent Diazobenzene Inhibitors for the BET Bromodomains
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November 2013 |
Discovery of Benzotriazolo[4,3- d ][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains
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March 2015 |
Discovery of Benzo[ cd ]indol-2(1 H )-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation
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April 2015 |
BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen
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June 2017 |
Design and Optimization of Benzopiperazines as Potent Inhibitors of BET Bromodomains
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July 2017 |
Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors
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December 2017 |
Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors
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March 2017 |
Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain
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April 2018 |
Structure-Based Discovery and Optimization of Benzo[ d ]isoxazole Derivatives as Potent and Selective BET Inhibitors for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC)
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March 2018 |
Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9 H -pyrimido[4,5- b ]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor
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March 2017 |
Structure-Based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors
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March 2015 |
BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells
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May 2015 |
Privileged Diazepine Compounds and Their Emergence as Bromodomain Inhibitors
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May 2014 |
Protacs: Chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradation
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July 2001 |
Chemical Inducers of Targeted Protein Degradation
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April 2010 |
Small molecule-mediated protein knockdown as a new approach to drug discovery
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January 2016 |
Small-Molecule PROTACS: New Approaches to Protein Degradation
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January 2016 |
Proteolysis-Targeting Chimeras: Induced Protein Degradation as a Therapeutic Strategy
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March 2017 |
Waste disposal—An attractive strategy for cancer therapy
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March 2017 |
You can glue it too!
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April 2017 |
Small-Molecule-Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging
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June 2015 |
Jostling for Position: Optimizing Linker Location in the Design of Estrogen Receptor-Targeting PROTACs
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May 2010 |
Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy
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February 2012 |
Catalytic in vivo protein knockdown by small-molecule PROTACs
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June 2015 |
Development of BCR-ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand
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October 2016 |
Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL
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November 2015 |
Phthalimide conjugation as a strategy for in vivo target protein degradation
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May 2015 |
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression
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March 2017 |
Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer
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February 2017 |
BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment
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July 2017 |
PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer
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June 2016 |
Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4
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June 2015 |
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4
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June 2015 |
RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain
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November 2013 |
Identification of a Primary Target of Thalidomide Teratogenicity
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March 2010 |
Structure of the DDB1–CRBN E3 ubiquitin ligase in complex with thalidomide
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July 2014 |
Structure of the human Cereblon–DDB1–lenalidomide complex reveals basis for responsiveness to thalidomide analogs
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August 2014 |
BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc
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September 2011 |
A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase
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June 2016 |
Development and validation of a genetic algorithm for flexible docking 1 1Edited by F. E. Cohen
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April 1997 |
Improved protein-ligand docking using GOLD
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August 2003 |