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| 36966198 | Endogenous bioluminescent reporters reveal a sustained increase in utrophin gene expression upon EZH2 and ERK1/2 inhibition. | Commun Biol | 2023 |
| 37967462 | Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N-Terminal Bromodomain Chemical Probe. | J Med Chem | 2023 |
| 37736196 | Design and Characterization of 1,3-Dihydro-2<i>H</i>-benzo[<i>d</i>]azepin-2-ones as Rule-of-5 Compliant Bivalent BET Inhibitors. | ACS Med Chem Lett | 2023 |
| 37060086 | Bromodomain inhibitor i-BET858 triggers a unique transcriptional response coupled to enhanced DNA damage, cell cycle arrest and apoptosis in high-grade ovarian carcinoma cells. | Clin Epigenetics | 2023 |
| 37024615 | Drug-induced loss of imprinting revealed using bioluminescent reporters of Cdkn1c. | Sci Rep | 2023 |
| 37120667 | In silico enhancer mining reveals SNS-032 and EHMT2 inhibitors as therapeutic candidates in high-grade serous ovarian cancer. | Br J Cancer | 2023 |
| 37232738 | The Epigenetic Reader Protein SP140 Regulates Dendritic Cell Activation, Maturation and Tolerogenic Potential. | Curr Issues Mol Biol | 2023 |
| 34773923 | A randomized study of the safety and pharmacokinetics of GSK3358699, a mononuclear myeloid-targeted bromodomain and extra-terminal domain inhibitor. | Br J Clin Pharmacol | 2022 |
| 35831302 | Bromodomain factor 5 is an essential regulator of transcription in Leishmania. | Nat Commun | 2022 |
| 35426377 | Combined noncanonical NF-κB agonism and targeted BET bromodomain inhibition reverse HIV latency ex vivo. | J Clin Invest | 2022 |
| 35655123 | Phase 1 and preclinical profiling of ESM-HDAC391, a myeloid-targeted histone deacetylase inhibitor, shows enhanced pharmacology and monocytopaenia. | Br J Clin Pharmacol | 2022 |
| 35619690 | Bromodomain Inhibitors Modulate FcγR-Mediated Mononuclear Phagocyte Activation and Chemotaxis. | Front Immunol | 2022 |
| 35482332 | Essential Bromodomain <i>Tc</i>BDF2 as a Drug Target against Chagas Disease. | ACS Infect Dis | 2022 |
| 36176467 | <i>N-</i>terminal BET bromodomain inhibitors disrupt a BRD4-p65 interaction and reduce inducible nitric oxide synthase transcription in pancreatic β-cells. | Front Endocrinol (Lausanne) | 2022 |
| 36139421 | A BET Protein Inhibitor Targeting Mononuclear Myeloid Cells Affects Specific Inflammatory Mediators and Pathways in Crohn's Disease. | Cells | 2022 |
| 35896525 | Cohesin couples transcriptional bursting probabilities of inducible enhancers and promoters. | Nat Commun | 2022 |
| 36378954 | Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432. | J Med Chem | 2022 |
| 35239184 | Selective inhibitors of bromodomain BD1 and BD2 of BET proteins modulate radiation-induced profibrotic fibroblast responses. | Int J Cancer | 2022 |
| 34633041 | Carboxylesterase-1 Assisted Targeting of HDAC Inhibitors to Mononuclear Myeloid Cells in Inflammatory Bowel Disease. | J Crohns Colitis | 2022 |
| 33005945 | Tyrosine Kinase 2 Signalling Drives Pathogenic T cells in Colitis. | J Crohns Colitis | 2021 |
| 33619107 | Bromodomain proteins regulate human cytomegalovirus latency and reactivation allowing epigenetic therapeutic intervention. | Proc Natl Acad Sci U S A | 2021 |
| 33662213 | Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors. | J Med Chem | 2021 |
| 34612618 | Expanding Bromodomain Targeting into Neglected Parasitic Diseases. | ACS Infect Dis | 2021 |
| 34387088 | Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression. | J Med Chem | 2021 |
| 34413961 | Optimization of Naphthyridones into Selective TATA-Binding Protein Associated Factor 1 (TAF1) Bromodomain Inhibitors. | ACS Med Chem Lett | 2021 |
| 34251219 | Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit. | J Med Chem | 2021 |
| 33968050 | Novel Insights Into Rheumatoid Arthritis Through Characterization of Concordant Changes in DNA Methylation and Gene Expression in Synovial Biopsies of Patients With Differing Numbers of Swollen Joints. | Front Immunol | 2021 |
| 34039605 | BRD4 methylation by the methyltransferase SETD6 regulates selective transcription to control mRNA translation. | Sci Adv | 2021 |
| 34233910 | IFN-γ Drives Human Monocyte Differentiation into Highly Proinflammatory Macrophages That Resemble a Phenotype Relevant to Psoriasis. | J Immunol | 2021 |
| 34260229 | Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors. | J Med Chem | 2021 |
| 34232650 | Identification of a Series of <i>N</i>-Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins. | J Med Chem | 2021 |
| 34255512 | Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors. | J Med Chem | 2021 |
| 32193360 | Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. | Science | 2020 |
| 33490899 | Brd2/4 and Myc regulate alternative cell lineage programmes during early osteoclast differentiation in vitro. | iScience | 2020 |
| 31813765 | Epigenetic Regulation of T Cell Memory: Recalling Therapeutic Implications. | Trends Immunol | 2020 |
| 31904959 | Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening. | J Med Chem | 2020 |
| 31971998 | Efficacy of combined CDK9/BET inhibition in preclinical models of MLL-rearranged acute leukemia. | Blood Adv | 2020 |
| 32862441 | The catalytic domain of the histone methyltransferase NSD2/MMSET is required for the generation of B1 cells in mice. | FEBS Lett | 2020 |
| 32691589 | GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins. | J Med Chem | 2020 |
| 32832027 | GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family. | ACS Med Chem Lett | 2020 |
| 32702236 | The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor. | J Med Chem | 2020 |
| 32787145 | Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype. | J Med Chem | 2020 |
| 32123118 | Histone H3K27me3 demethylases regulate human Th17 cell development and effector functions by impacting on metabolism. | Proc Natl Acad Sci U S A | 2020 |
| 32410449 | 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. | J Med Chem | 2020 |
| 32321240 | Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode. | J Med Chem | 2020 |
| 30514804 | Lysine specific demethylase 1 inactivation enhances differentiation and promotes cytotoxic response when combined with all-<i>trans</i> retinoic acid in acute myeloid leukemia across subtypes. | Haematologica | 2019 |
| 31736752 | Targeting Histone Deacetylases in Myeloid Cells Inhibits Their Maturation and Inflammatory Function With Limited Effects on Atherosclerosis. | Front Pharmacol | 2019 |
| 32328561 | Phase 1 Study of Molibresib (GSK525762), a Bromodomain and Extra-Terminal Domain Protein Inhibitor, in NUT Carcinoma and Other Solid Tumors. | JNCI Cancer Spectr | 2019 |
| 31266503 | BRD4 bimodal binding at promoters and drug-induced displacement at Pol II pause sites associates with I-BET sensitivity. | Epigenetics Chromatin | 2019 |
| 31257072 | Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss. | Cancer Cell | 2019 |