66 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain.
Pfizer
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
Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors.
Ludwig-Maximilians-Universit£T M£Nchen
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).
Constellation Pharmaceuticals
The"Gatekeeper" Residue Influences the Mode of Binding of Acetyl Indoles to Bromodomains.
University Of Z£Rich
Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.
Genentech
KATching-Up on Small Molecule Modulators of Lysine Acetyltransferases.
University Of Freiburg
Discovery of CREBBP Bromodomain Inhibitors by High-Throughput Docking and Hit Optimization Guided by Molecular Dynamics.
University Of Z£Rich
Fragment-Based Design of Selective Nanomolar Ligands of the CREBBP Bromodomain.
University Of Z£Rich
Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.
Shandong University
Structure-Based Design of¿-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors.
University Of Michigan
A novel cell-permeable, selective, and noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular pruning/classical isosterism approach.
Universit£
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.
Glaxosmithkline
Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains.
Icahn School Of Medicine At Mount Sinai
Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.
University Of Oxford
Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.
Pfizer
Discovery and characterization of small molecule inhibitors of the BET family bromodomains.
Glaxosmithkline
Development of live-cell imaging probes for monitoring histone modifications.
Japan Science And Technology Agency
3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
University Of Oxford
Rapid identification of improved protein ligands using peptoid microarrays.
University Of Texas Southwestern Medical Center
Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153).
Astrazeneca
Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.
Genentech
Histone acetyltransferase inhibitors: An overview in synthesis, structure-activity relationship and molecular mechanism.
Sichuan University
Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
University Of Texas Medical Branch
Small-Molecule Modulators of the Hypoxia-Inducible Factor Pathway: Development and Therapeutic Applications.
China Pharmaceutical University
Systematically Mitigating the p38? Activity of Triazole-based BET Inhibitors.
University Of Minnesota Twin Cities
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
A Qualified Success: Discovery of a New Series of ATAD2 Bromodomain Inhibitors with a Novel Binding Mode Using High-Throughput Screening and Hit Qualification.
Cellzome
GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like.
Genentech
[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains.
University Of Oxford
Identification of novel inhibitors of histone acetyltransferase hMOF through high throughput screening.
Chinese Academy Of Sciences
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.
Universitaire Vaudois
Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors.
Chinese Academy Of Sciences
Binding Motifs in the CBP Bromodomain: An Analysis of 20 Crystal Structures of Complexes with Small Molecules.
University Of Zurich
Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
University Of Strathclyde
Theoretical research in structure characteristics of different inhibitors and differences of binding modes with CBP bromodomain.
Jilin University
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
Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer.
Chinese Academy Of Sciences
Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
University Of Texas Medical Branch
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
Discovery of Spiro Oxazolidinediones as Selective, Orally Bioavailable Inhibitors of p300/CBP Histone Acetyltransferases.
Abbvie
BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.
University Of Oxford
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
Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains.
Bayer
Drug Discovery Targeting Bromodomain-Containing Protein 4.
University Of Texas Medical Branch
A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.
Genentech
Virtual screen to NMR (VS2NMR): Discovery of fragment hits for the CBP bromodomain.
University Of Z£Rich
Multiple histamine receptors: properties and functional characteristics.
Queen'S Medical Centre
Anthranilimide based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes. Part 3: X-ray crystallographic characterization, core and urea optimization and in vivo efficacy.
Gsk
Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs.
Kochi Medical School