Patricia A. Elkins

TL;DR: 2,4-Difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3- pyridinyl}benzenesulfonamide (GSK2126458, 1) has been identified as a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models.

TL;DR: The hypothesis that bacterial enoyl-ACP reductases are valid targets for antibacterial agents is supported, with a new series of inhibitors developed with greatly increased potency against FabI-containing organisms.

TL;DR: Comparison with the crystal structure of the most closely related MMP, MMP2, indicates that the conformations of residues in the active-site cleft and in the cysteine-switch peptide of the prodomain are highly conserved and that design of MMP9-specific inhibitors will be challenging.

TL;DR: Mutational analyses demonstrate that the knot is important for AdoMet binding and catalytic activity, and that the C-terminal domain is not only required for tRNA binding but plays a functional role in catalyticActivity.

TL;DR: The 2014 CSAR Benchmark Exercise was the last community-wide exercise conducted by the group at the University of Michigan, Ann Arbor, and GlaxoSmithKline donated unpublished crystal structures and affinity data from in-house projects, which lends greater statistical significance to comparisons between different methods.