John J G Tesmer
Affiliation: Purdue University
Beyett T, Gan X, Reilly S, Chang L, Gomez A, Saltiel A, et al
. Carboxylic Acid Derivatives of Amlexanox Display Enhanced Potency toward TBK1 and IKK? and Reveal Mechanisms for Selective Inhibition. Mol Pharmacol. 2018;94:1210-1219 pubmed publisher
..The structure-activity relationships and cocrystal structures described herein will aid in future structure-guided inhibitor development using the amlexanox pharmacophore for the treatment of obesity and type 2 diabetes. ..
Manthei K, Ahn J, Glukhova A, Yuan W, Larkin C, Manett T, et al
. A retractable lid in lecithin:cholesterol acyltransferase provides a structural mechanism for activation by apolipoprotein A-I. J Biol Chem. 2017;292:20313-20327 pubmed publisher
..These data suggest a model wherein the active site of LCAT is shielded from soluble substrates by a dynamic lid until it interacts with HDL to allow transesterification to proceed. ..
Bouley R, Waldschmidt H, Cato M, Cannavo A, Song J, Cheung J, et al
. Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors. Mol Pharmacol. 2017;92:707-717 pubmed publisher
..This conformation is analogous to one that can be assumed by GRK5, at least partially explaining the loss in selectivity. ..