Discovery of a brain-permeable bromodomain and extra terminal domain (BET) inhibitor with selectivity for BD1 for the treatment of multiple sclerosis

Multiple sclerosis genomic map implicates peripheral immune cells and microglia in susceptibility

Nikolaos A. Patsopoulos, Sergio E. Baranzini, Adam Santaniello et al. · Science · 2019 · 1.4K citations · Full text

Life Sciences, Genetics, Immunology +17

Target validation using chemical probes

Mark E. Bunnage, Eugene L. Piatnitski Chekler, Lyn H. Jones · Nature Chemical Biology · 2013 · 435 citations

Pharmacy, Medicinal Chemistry, Pharmacology +13

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation

Omer Gilan, Inmaculada Rioja, Kathy Knezevic et al. · Science · 2020 · 428 citations · Full text

Life Sciences, Immunology, Pharmacology +13

Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

Emily J. Faivre, Keith F. McDaniel, Daniel H. Albert et al. · Nature · 2020 · 404 citations

Life Sciences, Molecular Biology, Oncology +10

Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials

Brian K. Albrecht, Victor Gehling, Michael C. Hewitt et al. · Journal of Medicinal Chemistry · 2016 · 215 citations · Full text

Medicine, Oncology, Pharmacology +15