Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains

Olivier Mirguet, Romain Gosmini, Jérôme Toum, +20

Journal of Medicinal Chemistry

Histone ModificationsChemoprevention StrategyEpigenetic ChangeGeneticsMolecular Biology +20

Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy

S. Picaud, O. Fedorov, Angeliki Thanasopoulou, +34

Cancer Research

BET Inhibition Silences Expression of MYCN and BCL2 and Induces Cytotoxicity in Neuroblastoma Tumor Models

Anastasia Wyce, Gopinath Ganji, Kimberly N. Smitheman, +16

PLoS ONE

Mycn Copy NumberBet Family ProteinsCell RegulationOncogenic AgentMedicine +12

Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762

Aristeidis Chaidos, Valentina S. Caputo, Katerina Gouvedenou, +22

Blood

Phase 1 Study of Molibresib (GSK525762), a Bromodomain and Extra-Terminal Domain Protein Inhibitor, in NUT Carcinoma and Other Solid Tumors

Sarina A. Piha‐Paul, Christine L. Hann, Christopher A. French, +22

JNCI Cancer Spectrum

Selective inhibition of CD4 ⁺ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors

Hozefa S. Bandukwala, John D Gagnon, Susan Togher, +11

Proceedings of the National Academy of Sciences

Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease

Kenneth Down, Augustin Amour, Ian T. Baldwin, +21

Journal of Medicinal Chemistry

AsthmaAcute Lung InjuryPi3kδ PotencyInflammatory Lung DiseaseLung Inflammation +22

Long‐term changes in bone mineral density and predicted fracture risk in patients receiving androgen‐deprivation therapy for prostate cancer, with stratification of treatment based on presenting values

Vivek K. Wadhwa, Robin Weston, Rahul Mistry, +1

British Journal of Urology

The structure based design of dual HDAC/BET inhibitors as novel epigenetic probes

Stephen J. Atkinson, Peter E. Soden, Davina C. Angell, +11

MedChemComm

Epigenetic ChangeMolecular BiologyEpigeneticsNucleic Acid BiomarkersTumor Biology +20

Guidance for the assessment and management of prostate cancer treatment-induced bone loss. A consensus position statement from an expert group

Janet E. Brown, Catherine Handforth, Juliet Compston, +13

Journal of bone oncology