97 articles for thisTarget
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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
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.
University of Salerno
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
Acetyl-Click Screening Platform Identifies Small-Molecule Inhibitors of Histone Acetyltransferase 1 (HAT1).
Wayne State University
Recent Advances on Small-Molecule Bromodomain-Containing Histone Acetyltransferase Inhibitors.
Sichuan University
A novel pan-selective bromodomain inhibitor for epigenetic drug design.
Albert-Ludwigs-Universit£T Freiburg
Discovery and Characterization of Active CBP/EP300 Degraders Targeting the HAT Domain.
University of Zurich
Discovery of Exceptionally Potent, Selective, and Efficacious PROTAC Degraders of CBP and p300 Proteins.
University of Michigan
Privileged heterocycles for DNA-encoded library design and hit-to-lead optimization.
Chinese Academy of Sciences
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
Research progress of dual inhibitors targeting crosstalk between histone epigenetic modulators for cancer therapy.
Xinxiang Medical University
Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate.
Glaxosmithkline R&D
Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer.
Guangzhou Medical University
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, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.
Md Anderson Cancer Center
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
Controlling Intramolecular Interactions in the Design of Selective, High-Affinity Ligands for the CREBBP Bromodomain.
University of Oxford
Development of Dimethylisoxazole-Attached Imidazo[1,2-
University of Massachusetts Boston
Discovery of benzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivatives as orally available bromodomain and extra-terminal domain (BET) inhibitors with efficacy in an in vivo psoriatic animal model.
Kyorin Pharmaceutical
Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains.
Constellation Pharmaceuticals
Structure-based drug optimization and biological evaluation of tetrahydroquinolin derivatives as selective and potent CBP bromodomain inhibitors.
Chinese Academy of Sciences
Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition.
Glaxosmithkline R&D
Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.
University of Oxford
Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.
University of Oxford
CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses.
University of Oxford
Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor.
Constellation Pharmaceuticals
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
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
Systematically Mitigating the p38α 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
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
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
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
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
PROTEIN-PROTEIN INTERACTION MODULATORS OF AURORA KINASE A AND THEIR USE IN THE PREVENTION AND/OR TREATMENT OF CANCER
Eberhard Karls Universitat Tubingen
Compound as selective JAK inhibitor, and salt and therapeutic use thereof
Suzhou Longbiotech Pharmaceuticals
Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides
Pfizer
Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
Enanta Pharmaceuticals
Quinoxaline compounds as type III receptor tyrosine kinase inhibitors
Development Center For Biotechnology
Validation of flavonoids as potential dipeptidyl peptidase III inhibitors: Experimental and computational approach.
Josip Juraj Strossmayer University of Osijek
Discovery of imidazopyridine derivatives as novel c-Met kinase inhibitors: Synthesis, SAR study, and biological activity.
China Pharmaceutical University
Perfluoro-tert-butyl Homoserine Is a Helix-Promoting, Highly Fluorinated, NMR-Sensitive Aliphatic Amino Acid: Detection of the Estrogen Receptor·Coactivator Protein-Protein Interaction by (19)F NMR.
University of Delaware
Metronidazole containing pyrazole derivatives potently inhibit tyrosyl-tRNA synthetase: design, synthesis, and biological evaluation.
Nanjing University
Neuroprotective and neuro-restorative iron chelators and monoamine oxidase inhibitors and uses thereof
TBA
Spiro[9,10-dihydroanthracene]-9,3'-pyrrolidine-a structurally unique tetracyclic 5-HT2A receptor antagonist.
Virginia Commonwealth University