53 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
Organization
Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe.
Glaxosmithkline
Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening.
University of Dundee
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.
Genentech
KATching-Up on Small Molecule Modulators of Lysine Acetyltransferases.
University of Freiburg
Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain.
University of Oxford
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.
Glaxosmithkline
A novel cell-permeable, selective, and noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular pruning/classical isosterism approach.
University of Salerno
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.
Glaxosmithkline
Azide-alkyne cycloaddition affording enzymatically tunable bisubstrate based inhibitors of histone acetyltransferase PCAF.
Utrecht University
Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains.
Icahn School of Medicine At Mount Sinai
Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions.
University of Oxford
Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs).
The Institute of Cancer Research
6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site.
University of Groningen
Synthesis and biological testing of novel pyridoisothiazolones as histone acetyltransferase inhibitors.
Albert-Ludwigs-University of Freiburg
Improved inhibition of the histone acetyltransferase PCAF by an anacardic acid derivative.
Groningen Research Institute of Pharmacy
Reactivity of isothiazolones and isothiazolone-1-oxides in the inhibition of the PCAF histone acetyltransferase.
University of Groningen
Inhibition of the PCAF histone acetyl transferase and cell proliferation by isothiazolones.
University of Groningen
Recent Advances on Small-Molecule Bromodomain-Containing Histone Acetyltransferase Inhibitors.
Sichuan University
First-in-Class Selective Inhibitors of the Lysine Acetyltransferase KAT8.
Sapienza University of Rome
Discovery of DS-9300: A Highly Potent, Selective, and Once-Daily Oral EP300/CBP Histone Acetyltransferase Inhibitor.
Daiichi Sankyo Co.
Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.
Genentech
Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials.
Constellation Pharmaceuticals
From Hit Seeking to Magic Bullets: The Successful Union of Epigenetic and Fragment Based Drug Discovery (EPIDD + FBDD).
University of S£O Paulo
Discovery of EP300/CBP histone acetyltransferase inhibitors through scaffold hopping of 1,4-oxazepane ring.
Daiichi Sankyo
Structure-activity relationship and antitumor activity of 1,4-pyrazine-containing inhibitors of histone acetyltransferases P300/CBP.
Baylor College of Medicine
Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models.
Astrazeneca
Design, synthesis and biological evaluation of a novel spiro oxazolidinedione as potent p300/CBP HAT inhibitor for the treatment of ovarian cancer.
China Pharmaceutical University
4-Pyridone-3-carboxylic acid as a benzoic acid bioisostere: Design, synthesis, and evaluation of EP300/CBP histone acetyltransferase inhibitors.
Daiichi Sankyo
From triazolophthalazines to triazoloquinazolines: A bioisosterism-guided approach toward the identification of novel PCAF inhibitors with potential anticancer activity.
Al-Azhar University
New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition.
University of Minnesota
Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.
University of Oxford
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.
Glaxosmithkline R&D
Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.
University of Illinois At Chicago
Histone acetyltransferase inhibitors: An overview in synthesis, structure-activity relationship and molecular mechanism.
Sichuan University
Discovery of Pyrrolo[3,2- d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell-Active Inhibitors of P300/CBP-Associated Factor Bromodomain.
Sichuan University
Discovery, Structure-Activity Relationship, and Biological Activity of Histone-Competitive Inhibitors of Histone Acetyltransferases P300/CBP.
Avera Institute For Human Genetics
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.
Gilead Sciences
Discovery of Highly Potent, Selective, and Orally Efficacious p300/CBP Histone Acetyltransferases Inhibitors.
Chinese Academy of Sciences
Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors.
Chinese Academy of Sciences
Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
University of Strathclyde
Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300.
Wuxi Apptec
Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor.
University of Michigan
Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor.
TBA
Discovery and optimization of 1-(1H-indol-1-yl)ethanone derivatives as CBP/EP300 bromodomain inhibitors for the treatment of castration-resistant prostate cancer.
Guangzhou Medical University
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).
Genentech
Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies.
University College London
Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.
Abbvie
