Eric Boursier

TL;DR: X-ray crystal structures of compounds bound into bromodomains of Brd2 and Brd4 elucidate the molecular interactions of binding and explain the precisely defined stereochemistry required for activity.

TL;DR: This work describes the identification of a novel tetrahydroquinoline series through up-regulation of apolipoprotein A1 and the optimization into potent compounds active in murine models of septic shock and neuroblastoma, and reveals the interactions explaining the structure-activity relationships of binding.

TL;DR: The discovery, synthesis and biological evaluation of a novel series of 7-isoxazoloquinolines is described and several analogs are shown to increase ApoA1 expression within the nanomolar range in the human hepatitis cell line HepG2.

TL;DR: A novel compound library synthesized via on-DNA Suzuki-Miyaura cross-coupling and a protein crystal structure of 15e revealed that it binds to BCATm within the catalytic site adjacent to the PLP cofactor provided a good starting point for future structure-based discovery ofBCATm inhibitors.

TL;DR: X-ray structure revealed that 8b binds to the active site of BACTm in a unique mode via multiple H-bond and van der Waals interactions, which led to the discovery of a highly potent and selective compound, 1-(3-(5-bromothiophene- 2-carboxamido)cyclohexyl)-N-methyl-2-(pyridin-2-yl)-1H-benzo[d]imidazole-