Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof

Ryan R. Davis, Baoli Li, Sang Y. Yun, +8

Journal of Medicinal Chemistry

Janus Kinase 2Chemical BiologyPharmaceutical ChemistryTumor BiologyRheumatoid Disorder +20

Structural Basis of Inhibitor Selectivity in the BRD7/9 Subfamily of Bromodomains

Rezaul M. Karim, A. Chan, J. Zhu, +1

Journal of Medicinal Chemistry

Inhibitor SelectivityMolecular BiologyProtein 9Medicinal ChemistryStructure Elucidation +19

New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition

Huda Zahid, Caroline R. Buchholz, Manjulata Singh, +10

Journal of Medicinal Chemistry

The Crystal Structure of Fe₄S₄ Quinolinate Synthase Unravels an Enzymatic Dehydration Mechanism That Uses Tyrosine and a Hydrolase-Type Triad

Mickaël V. Cherrier, A. Chan, Claudine Darnault, +4

Journal of the American Chemical Society

Crystal StructureAldo-keto ReductaseMolecular BiologyChemical BiologyEnzymatic Modification +17

Studies of Inhibitor Binding to the [4Fe‐4S] Cluster of Quinolinate Synthase

A. Chan, Martin Clémancey, Jean‐Marie Mouesca, +4

Angewandte Chemie International Edition

New inhibitors for the BPTF bromodomain enabled by structural biology and biophysical assay development

Peter D. Ycas, Huda Zahid, A. Chan, +5

Organic & Biomolecular Chemistry

Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors

Rezaul M. Karim, Melissa J. Bikowitz, A. Chan, +7

Journal of Medicinal Chemistry

Drug TargetKinase InhibitorsMolecular BiologyChemical BiologyMedicinal Chemistry +15

IKKγ-Mimetic Peptides Block the Resistance to Apoptosis Associated with Kaposi's Sarcoma-Associated Herpesvirus Infection

Louise C. Briggs, A. Chan, Christopher Davis, +7

Journal of Virology

NMR Analyses of Acetylated H2A.Z Isoforms Identify Differential Binding Interactions with the Bromodomain of the NURF Nucleosome Remodeling Complex

Noelle M. Olson, Samantha Kroc, Jorden A. Johnson, +7

Biochemistry

Histone ModificationsMolecular RegulationEpigenetic ChangeMolecular BiologyEpigenetics +19

Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity

Xianghong Guan, Narsihmulu Cheryala, Rezaul M. Karim, +5

Journal of Medicinal Chemistry

Drug TargetProtein AssemblyProtein Conformational PlasticityMolecular BiologyExtraterminal Domain +14