Shiyao Xu

TL;DR: MK-8722 is developed, a potent, direct, allosteric activator of all 12 mammalian AMPK complexes that induced robust, durable, insulin-independent glucose uptake and glycogen synthesis, with resultant improvements in glycemia and no evidence of hypoglycemia in rodents and rhesus monkeys.

TL;DR: The data indicate that sitagliptin is unlikely to be a perpetrator of drug-drug interactions with Pgp, hOAT1, or hOat3 substrates at clinically relevant concentrations, and the effects may not be clinically meaningful, due to the high safety margin of sitgliptin.

TL;DR: The metabolism and excretion of [14C]sitagliptin, an orally active, potent and selective dipeptidyl peptidase 4 inhibitor, were investigated in humans after a single oral dose of 83 mg/193 μCi, indicating that sitagli leptin was eliminated primarily by renal excretion.

TL;DR: A radiolabeled fluoroolefin 33 was shown to possess a high propensity to form reactive metabolites, thus revealing a potential liability for this class of DPP-4 inhibitors.

TL;DR: This communication highlights a strategy leveraging small molecule active site dimers to inhibit the large symmetric binding pocket in the STING protein, which exhibits good oral exposure, slow binding kinetics, and functional inhibition of STING-mediated cytokine release.