Jason Witherington

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

Olivier Mirguet, Romain Gosmini, Jérôme Toum et al. · Journal of Medicinal Chemistry · 2013 · 304 citations · Full text

Medicine, Medicinal Chemistry, Pharmacology +17

GSK189254, a Novel H3 Receptor Antagonist That Binds to Histamine H3 Receptors in Alzheimer’s Disease Brain and Improves Cognitive Performance in Preclinical Models

Andrew D. Medhurst, A.R. Atkins, I.J.M. Beresford et al. · Journal of Pharmacology and Experimental Therapeutics · 2007 · 301 citations

Medicine, Medicinal Chemistry, Pharmacology +13

Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A)

Jonathan T. Seal, Yann Lamotte, Frédéric Donche et al. · Bioorganic & Medicinal Chemistry Letters · 2012 · 213 citations · Full text

Life Sciences, Medicinal Chemistry, Pharmacology +16

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

Aristeidis Chaidos, Valentina S. Caputo, Katerina Gouvedenou et al. · Blood · 2013 · 202 citations

Pharmacy, Medicinal Chemistry, Pharmacology +6

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 et al. · Proceedings of the National Academy of Sciences · 2012 · 185 citations · Full text

Life Sciences, Cell Biology, Immunology +17