67 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 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
KATching-Up on Small Molecule Modulators of Lysine Acetyltransferases.
University of Freiburg
Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.
Shandong University
A novel cell-permeable, selective, and noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular pruning/classical isosterism approach.
Universit£
PAINS in the assay: chemical mechanisms of assay interference and promiscuous enzymatic inhibition observed during a sulfhydryl-scavenging HTS.
Mayo Clinic
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.
Glaxosmithkline
Pharmacophore-based virtual screening and biological evaluation of small molecule inhibitors for protein arginine methylation.
Georgia State University
Binding Model for the Interaction of Anticancer Arylsulfonamides with the p300 Transcription Cofactor.
TBA
Design and in vitro activities of N-alkyl-N-[(8-R-2,2-dimethyl-2H-chromen-6-yl)methyl]heteroarylsulfonamides, novel, small-molecule hypoxia inducible factor-1 pathway inhibitors and anticancer agents.
Emory University
Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs).
The Institute of Cancer Research
Mechanism of p300 specific histone acetyltransferase inhibition by small molecules.
Jawaharlal Nehru Centre For Advanced Scientific Research
6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site.
University of Groningen
Computer- and structure-based lead design for epigenetic targets.
Martin-Luther University of Halle-Wittenberg
Discovery and mechanistic study of a class of protein arginine methylation inhibitors.
Georgia State University
Cinnamoyl compounds as simple molecules that inhibit p300 histone acetyltransferase.
Sapienza University of Rome
Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.
Genentech
Research progress of dual inhibitors targeting crosstalk between histone epigenetic modulators for cancer therapy.
Xinxiang Medical University
Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening.
Glaxosmithkline
Diversity-oriented synthesis as a tool to expand the chemical space of DNA-encoded libraries.
University of Florence
Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate.
Glaxosmithkline R&D
Discovery of EP300/CBP histone acetyltransferase inhibitors through scaffold hopping of 1,4-oxazepane ring.
Daiichi Sankyo
Small molecule therapeutics for tauopathy in Alzheimer's disease: Walking on the path of most resistance.
Karolinska Institutet
Discovery of novel benzimidazole derivatives as potent p300 bromodomain inhibitors with anti-proliferative activity in multiple cancer cells.
Fudan University
Structure-activity relationship and antitumor activity of 1,4-pyrazine-containing inhibitors of histone acetyltransferases P300/CBP.
Baylor College of Medicine
An insight into the medicinal attributes of berberine derivatives: A review.
Isf College of Pharmacy
Discovery of Potent and Novel Dual PARP/BRD4 Inhibitors for Efficient Treatment of Pancreatic Cancer.
China Pharmaceutical University
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
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
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
Advances in inhibition of protein-protein interactions targeting hypoxia-inducible factor-1 for cancer therapy.
China Pharmaceutical University
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
Small-Molecule Modulators of the Hypoxia-Inducible Factor Pathway: Development and Therapeutic Applications.
China Pharmaceutical University
Discovery of Benzoylsulfonohydrazides as Potent Inhibitors of the Histone Acetyltransferase KAT6A.
Cancer Therapeutics Crc
Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors.
Fudan 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
Characterizing the Covalent Targets of a Small Molecule Inhibitor of the Lysine Acetyltransferase P300.
National Cancer Institute
Enzyme kinetics and inhibition of histone acetyltransferase KAT8.
University of Groningen
Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors.
Chinese Academy of Sciences
Antiproliferative and apoptotic activities of sequence-specific histone acetyltransferase inhibitors.
Kyoto University
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
Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins.
Temple University
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
Swinhoeisterols from the South China Sea Sponge Theonella swinhoei.
Second Military Medical University
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
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
