Robert Elling

TL;DR: a4−/− mice exhibit a profound accumulation of iron in splenic macrophages, which are critical for the reutilization of iron from engulfed red blood cells, and a previously unappreciated role for autophagy and NCOA4 in the control of iron homeostasis in vivo is revealed.

TL;DR: A saturation strategy focused on improving the selectivity and physicochemical properties of ATR inhibitor HTS hit 1 led to a novel series of highly potent and selective tetrahydropyrazolo[1,5-a]pyrazines.

TL;DR: In this article, the side chain hydrophobicity of the P4 residue of cyclophilin D has been reduced to preserve binding and antiviral potency while decreasing transporter inhibition.

TL;DR: This work structurally and mechanistically characterize LpxM, providing insights that may enable the targeted discovery of inhibitors that prevent lipid A maturation, and describes a high-throughput, label-free mass spectrometric assay to characterize acyltransferase enzymatic activity.

TL;DR: Imidazopyridine compound 1, a potent, selective, and orally available pan-PI3K inhibitor, was further optimized in order to achieve efficacy in a PTEN-deleted A2780 ovarian cancer mouse xenograft model.