The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27682507 |
167 |
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. |
Genentech |
26061247 |
71 |
Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. |
The University of Texas M.D. Anderson Cancer Center |
26230603 |
176 |
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors. |
Glaxosmithkline |
26080064 |
141 |
Structure-Based Design of¿-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors. |
University of Michigan |
25314271 |
44 |
Biased multicomponent reactions to develop novel bromodomain inhibitors. |
Dana-Farber Institute |
25249180 |
146 |
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. |
Glaxosmithkline |
27757418 |
27 |
Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia. |
University of Oxford |
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 |
27528113 |
117 |
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 |
27219867 |
94 |
Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains. |
Genentech |
32321240 |
179 |
Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode. |
University of Strathclyde |
30606676 |
83 |
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor. |
Gilead Sciences |
31398032 |
113 |
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 |
30289257 |
177 |
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 |
31620231 |
68 |
Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold. |
Dana Farber Cancer Institute |
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 |
28892380 |
93 |
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP). |
Genentech |
28740608 |
96 |
GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2). |
Genentech |
27935314 |
4 |
A Versatile Method to Determine the Cellular Bioavailability of Small-Molecule Inhibitors. |
H. Lee Moffitt Cancer Center and Research Institute |