34 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex.
University of Cambridge
Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.
Pfizer
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.
Glaxosmithkline
Design, synthesis and biological evaluation of 3-amino-6-(2-hydroxyphenyl)pyridazin-4-aryl derivatives as SMARCA2/4 degraders.
Sichuan University
Discovery of High-Affinity SMARCA2/4 Bromodomain Ligands and Development of Potent and Exceptionally Selective SMARCA2 PROTAC Degraders.
University of Michigan
SMARCA2 protein: Structure, function and perspectives of drug design.
Wuhan Institute of Technology
1,6-Naphthridine Compounds as SMARCA2 Inhibitors for Treating Non-small Cell Lung Cancer.
Smith, Gambrell & Russell
Discovery of FHD-286, a First-in-Class, Orally Bioavailable, Allosteric Dual Inhibitor of the Brahma Homologue (BRM) and Brahma-Related Gene 1 (BRG1) ATPase Activity for the Treatment of SWItch/Sucrose Non-Fermentable (SWI/SNF) Dependent Cancers.
Foghorn Therapeutics
Discovery of SMD-3236: A Potent, Highly Selective and Efficacious SMARCA2 Degrader for the Treatment of SMARC4-Deficient Human Cancers.
University of Michigan
Discovery of Potent, Highly Selective, and Efficacious SMARCA2 Degraders.
SK Life Science Labs
Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.
University of Cambridge
PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models.
Arvinas LLC
Exploitation of Proximity-Mediated Effects in Drug Discovery: An Update of Recent Research Highlights in Perturbing Pathogenic Proteins and Correlated Issues.
Anhui University of Chinese Medicine
Discovery of SMD-3040 as a Potent and Selective SMARCA2 PROTAC Degrader with Strong
University of Michigan
Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.
Genentech
Recent advances in epigenetic proteolysis targeting chimeras (Epi-PROTACs).
"Sapienza" University of Rome
GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1.
Constellation, A Morphosys
Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening.
Medical College of Wisconsin
Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models.
Astrazeneca
Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis.
Goethe University Frankfurt
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
Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.
Genentech
Systematically Mitigating the p38α Activity of Triazole-based BET Inhibitors.
University of Minnesota Twin Cities
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.
Gilead Sciences
Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers.
Novartis Institutes For Biomedical Research
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
Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor.
TBA
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
TRIAZINE DIONE DERIVATIVE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF IN MEDICINE
Jiangsu Hengrui Pharmaceuticals