John J G Tesmer


Affiliation: Purdue University
Country: USA


  1. Bandekar S, Arang N, Tully E, Tang B, Barton B, Li S, et al. Structure of the C-terminal guanine nucleotide exchange factor module of Trio in an autoinhibited conformation reveals its oncogenic potential. Sci Signal. 2019;12: pubmed publisher
    ..These mutations increase mitogenic signaling through the RhoA axis and, therefore, may represent cancer drivers operating in a Gαq/11-independent manner. ..
  2. 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 IKKε 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. ..
  3. 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. ..
  4. 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. ..