The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28002667 |
51 |
Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe. |
Glaxosmithkline |
27994766 |
28 |
Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening. |
University of Dundee |
27682507 |
167 |
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. |
Genentech |
26701186 |
50 |
KATching-Up on Small Molecule Modulators of Lysine Acetyltransferases. |
University of Freiburg |
26731131 |
2 |
Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain. |
University of Oxford |
26230603 |
176 |
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors. |
Glaxosmithkline |
25730130 |
20 |
A novel cell-permeable, selective, and noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular pruning/classical isosterism approach. |
Universit£ |
25249180 |
146 |
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. |
Glaxosmithkline |
24345448 |
4 |
Azide-alkyne cycloaddition affording enzymatically tunable bisubstrate based inhibitors of histone acetyltransferase PCAF. |
Utrecht University |
24144283 |
100 |
Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. |
Icahn School of Medicine At Mount Sinai |
22924434 |
4 |
Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions. |
University of Oxford |
19114310 |
30 |
Bisubstrate Inhibitors of the MYST HATs Esa1 and Tip60. |
Georgia State University |
19101154 |
28 |
Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs). |
The Institute of Cancer Research |
22100137 |
6 |
6-alkylsalicylates are selective Tip60 inhibitors and target the acetyl-CoA binding site. |
University of Groningen |
21353783 |
37 |
Synthesis and biological testing of novel pyridoisothiazolones as histone acetyltransferase inhibitors. |
Albert-Ludwigs-University of Freiburg |
20655754 |
2 |
Improved inhibition of the histone acetyltransferase PCAF by an anacardic acid derivative. |
Groningen Research Institute of Pharmacy |
19683843 |
16 |
Reactivity of isothiazolones and isothiazolone-1-oxides in the inhibition of the PCAF histone acetyltransferase. |
University of Groningen |
19111471 |
19 |
Inhibition of the PCAF histone acetyl transferase and cell proliferation by isothiazolones. |
University of Groningen |
27757418 |
27 |
Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia. |
University of Oxford |
32410449 |
88 |
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 |
32453591 |
70 |
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 |
31195169 |
46 |
Histone acetyltransferase inhibitors: An overview in synthesis, structure-activity relationship and molecular mechanism. |
Sichuan University |
30998845 |
58 |
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 |
32314924 |
44 |
Discovery, Structure-Activity Relationship, and Biological Activity of Histone-Competitive Inhibitors of Histone Acetyltransferases P300/CBP. |
Avera Institute For Human Genetics |
30606676 |
83 |
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor. |
Gilead Sciences |
31910017 |
43 |
Discovery of Highly Potent, Selective, and Orally Efficacious p300/CBP Histone Acetyltransferases Inhibitors. |
Chinese Academy of Sciences |
30297119 |
24 |
Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors. |
Chinese Academy of Sciences |
29656650 |
151 |
Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain. |
University of Strathclyde |
29169673 |
115 |
Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300. |
Wuxi Apptec |
28463487 |
185 |
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 |
30015487 |
96 |
Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor. |
TBA |
29448139 |
117 |
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 |
28527406 |
61 |
The relevance of K |
University of Groningen |
28892380 |
93 |
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP). |
Genentech |
28068087 |
80 |
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 |
28268136 |
130 |
Methylpyrrole inhibitors of BET bromodomains. |
Abbvie |
28949521 |
88 |
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 |