Francis Bourbonais

TL;DR: 19 is identified as a potent glucokinase activator with a greater than 50-fold liver-to-pancreas ratio of tissue distribution in rodent and non-rodent species, leading to its selection as a clinical development candidate for treating type 2 diabetes.

TL;DR: A unique metabolic liability of the 4-sulfonyl-2-pyridone ring system was identified wherein this heterocycle readily undergoes conjugation with glutathione under non-enzymatic conditions.

TL;DR: A novel series of spiroindoline-based inhibitors of Sky kinase that bind in the ATP-binding site and exhibit high levels of kinome selectivity through filling the Ala571-subpocket are discovered and exhibit moderate oral bioavailability in the rat.

TL;DR: This study compared the TPA-based quantitation of seven major hepatic uptake transporters in four human liver tissue samples using global proteomic data obtained from two multiplexed tandem mass tag experiments to the quantitative data from targeted proteomic assays.

TL;DR: It is demonstrated that both pyridone and pyrimidone heterocycles can be used as a potent donor-acceptor substituent and may find utility in other glucokinase activator series or beyond.