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Waldschmidt, H. V., Homan, K. T., Cato, M. C., Cruz-Rodríguez, O., Cannavo, A., Wilson, M. W., Song, J., Cheung, J. Y., Koch, W. J., Tesmer, J. J. G., Larsen, S. D. 2017. Structure-based design of highly selective and potent G protein-coupled receptor kinase 2 inhibitors based on paroxetine. J Med Chem. (Epub ahead of print.) doi: 10.1021/acs.jmedchem.7b00112.
Chen, Q., Tesmer, J. J. G. 2017. A receptor on acid. Cell 168:339-341.
Tesmer, J. J. G. 2016. Hitchhiking on the heptahelical highway: structure and function of 7TM receptor complexes. Nat Rev Mol Cell Biol. 17:439-450.
Yang, P., Homan, K. T., Li, Y., Cruz-Rodríguez, O., Tesmer, J. J. G., Chen, Z. 2016. Effect of lipid composition on membrane orientation of the G protein-coupled receptor kinase 2—Gβ1γ2 complex. Biochemistry 55:2841-2848.
Cash, J. N., Davis, E. M., Tesmer, J. J. G. 2016. Structural and biochemical characterization of the catalytic core of the metastatic factor P-Rex1 and its regulation by PtdIns(3,4,5)P3. Structure 24:730-740.
Wang, Y., Virtanen, J., Xue, Z., Tesmer, J. J. G., Zhang, Y. 2016. Using iterative fragment assembly and progressive sequence truncation to facilitate phasing and crystal structure determination of distantly related proteins. Acta Cryst D Struct Biol. 72:616-628.
Waldschmidt, H. V., Homan, K. T., Cruz-Rodríguez, O., Cato, M. C., Waninger-Saroni, J., Larimore, K. M., Cannavo, A., Song, J., Cheung, J. Y., Kirchhoff, P. D., Koch, W. J., Tesmer, J. J. G., Larsen, S. D. 2016. Structure-based design, synthesis and biological evaluation of highly selective and potent G protein-coupled receptor kinase 2 inhibitors. J Med Chem. 59:3793-3807.
Taylor, V. G., Bommarito, P. A., Tesmer, J. J. G. 2016. Structure of the regulator of G protein signaling 8 (RGS8)–Gαq complex: molecular basis for Gα selectivity. J Biol Chem. 291:5138-5145.
Abe, A., Hiraoka, M., Ohguro, H., Tesmer, J. J. G., Shayman, J. A. 2016. Preferential hydrolysis of truncated oxidized glycerophospholipids by lysosomal phospholipase A2. J Lipid Res. 58:339-349.
Homan, K. T., Waldschmidt, H. V., Glukhova, A., Cannavo, A., Song, J., Cheung, J. Y., Koch, W. J., Larsen, S. D., Tesmer, J. J. G. 2015. Crystal structure of G protein-coupled receptor kinase 5 in complex with a rationally designed inhibitor J Biol Chem. 290:20649-20659. (Selected as “Paper of the Week”)
Inagaki, S., Ghirlando, R., Vishnivetskiy, S. A., Homan, K. T., White, J. F., Tesmer, J. J. G., Gurevich, V. V., Grisshammer, R. 2015. G protein-coupled receptor kinase 2 (GRK2) and 5 (GRK5) exhibit selective phosphorylation of the neurotensin receptor in vitro. Biochemistry 54:4320-4329.
Li, L., Homan, K. T., Vishnivetskiy, S. A., Manglik, A., Tesmer, J. J. G., Gurevich, V. V., Gurevich, E. V. 2015. G protein-coupled receptor kinases of the GRK4 subfamily phosphorylate inactive G protein-coupled receptors (GPCRs). J Biol Chem. 290:10775-10790.
Azevedo, A. W., Doan, T., Moaven, H., Sokal, I., Baameur, F., Vishnivetskiy, S. A., Homan, K. T., Tesmer, J. J. G., Gurevich, V. V., Chen, J., Rieke, F. 2015. C-terminal threonines and serines play distinct roles in the desensitization of rhodopsin, a G protein-coupled receptor. Elife 4:e05981.
Schumacher, S. M., Gao, E., Zhu, W., Chen, X., Chuprun, J. K., Feldman, A. M., Tesmer, J. J. G., Koch, W. J. 2015. Paroxetine-mediated GRK2 inhibition reverses cardiac dysfunction and remodeling after myocardial infarction. Sci Transl Med. 7:277ra31.
Glukhova, A., Hinkovska-Galcheva, V., Kelly, R., Abe, A., Shayman, J. A., Tesmer, J. J. G. 2015. Structure and function of lysosomal phospholipase A2 and lecithin:cholesterol acyltransferase. Nat Commun. 6:6250.
Homan, K. T., Larimore, K. M., Elkins, J. M., Szklarz, M., Knapp, S., Tesmer, J. J. G. 2015. Identification and structure-function analysis of subfamily selective G protein-coupled receptor kinase inhibitors. ACS Chem Biol. 10:310-319.
Homan, K. T., Tesmer, J. J. G. 2015. Molecular basis for small molecule inhibition of G protein-coupled receptor kinases. ACS Chem Biol. 10:246-256.
Lyon, A. M., Begley, J. A., Manett, T. D., Tesmer, J. J. G. 2014. Molecular mechanisms of phospholipase C β3 autoinhibition. Structure 22:1844-1854.
Homan, K. T., Wu, E., Cannavo, A., Koch, W. J., Tesmer, J. J. G. 2014. Identification and characterization of amlexanox as a G protein-coupled receptor kinase 5 inhibitor. Molecules 19:16937-16949.
Beautrait, A., Michalski K. R., Lopez, T. S., Mannix, K. M., McDonald, D. J., Cutter, A. R., Medina, C. B., Hebert, A. M., Francis, C. J., Bouvier, M., Tesmer, J. J. G., Sterne-Marr, R. 2014. Mapping the putative G protein-coupled receptor (GPCR) docking site on GPCR kinase 2: insights from intact cell phosphorylation and recruitment assays. J Biol Chem. 289:25262-25275.
Swanson, C. J., Ritt, M., Wang, W., Lang, M. J., Narayan, A., Tesmer, J. J. G., Westfall, M., Sivaramakrishnan, S. 2014. Conserved modular domains team up to latch-open active protein kinase Cα. J Biol Chem. 289:17812-17829.
Homan, K. T., Tesmer, J. J. G. 2014. Structural insights into G protein-coupled receptor kinase function. Curr Opin Cell Biol. 27:25-31.
Homan K. T., Wu, E., Wilson, M. W., Singh, P., Larsen, S. D., Tesmer, J. J. G. 2014. Structural and functional analysis of G protein-coupled receptor kinase inhibition by paroxetine and a rationally designed analog. Mol Pharm. 85:237-248.
Ding, B., Glukhova, A., Sobczyk-Kojiro, K., Mosberg, H. I., Tesmer, J. J. G., Chen, Z. 2014. Unveiling the membrane-binding properties of N-terminal and C-terminal regions of G protein-coupled receptor kinase 5 by combined optical spectroscopies. Langmuir 30:823-831.
Lyon, A. M., Taylor, V. G., Tesmer, J. J. G. 2014. Strike a pose: Gαq complexes at the membrane. Trends Pharmacol Sci. 35:23-30.