Browse > Article
http://dx.doi.org/10.4062/biomolther.2016.262

Conceptual Progress for the Improvements in the Selectivity and Efficacy of G Protein-Coupled Receptor Therapeutics: An Overview  

Kim, Kyeong-Man (College of Pharmacy, Chonnam National University)
Publication Information
Biomolecules & Therapeutics / v.25, no.1, 2017 , pp. 1-3 More about this Journal
Keywords
Conformational change; Biased signaling; Insulin resistance; Bioinformatics; Viral G protein-coupled receptor; Sphingosine-1-phosphate;
Citations & Related Records
Times Cited By KSCI : 7  (Citation Analysis)
연도 인용수 순위
1 Furlong, M. and Seong, J. Y. (2017) Evolutionary and comparative genomics to drive rational drug design, with particular focus on neuropeptide seven-transmembrane receptors. Biomol. Ther. (Seoul) 25, 57-68.   DOI
2 Gilman, A. G. (1987) G proteins: transducers of receptor-generated signals. Annu. Rev. Biochem. 56, 615-649.   DOI
3 Lee, S., Chung, Y. H. and Lee, C. (2017) US28, a virally-encoded GPCR as an antiviral target for human cytomegalovirus infection. Biomol. Ther. (Seoul) 25, 69-79.   DOI
4 Agresti, J. J., Antipov, E., Abate, A. R., Ahn, K., Rowat, A. C., Baret, J. C., Marquez, M., Klibanov, A. M., Griffiths, A. D. and Weitz, D. A. (2010) Ultrahigh-throughput screening in drop-based microfluidics for directed evolution. Proc. Natl. Acad. Sci. U.S.A. 107, 4004-4009.   DOI
5 Bjarnadottir, T. K., Gloriam, D. E., Hellstrand, S. H., Kristiansson, H., Fredriksson, R. and Schioth, H. B. (2006) Comprehensive repertoire and phylogenetic analysis of the G protein-coupled receptors in human and mouse. Genomics 88, 263-273.   DOI
6 Nathans, J. and Hogness, D. S. (1983) Isolation, sequence analysis, and intron-exon arrangement of the gene encoding bovine rhodopsin. Cell 34, 807-814.   DOI
7 Lefkowitz, R. J. (2000) The superfamily of heptahelical receptors. Nat. Cell Biol. 2, E133-E136.   DOI
8 Lefkowitz, R. J. and Haber, E. (1971) A fraction of the ventricular myocardium that has the specificity of the cardiac ${\beta}$-adrenergic receptor. Proc. Natl. Acad. Sci. U.S.A. 68, 1773-1777.   DOI
9 Mangmool, S., Denkaew, T., Parichatikanond, W. and Kurose, H. (2017) ${\beta}$-adrenergic receptor and insulin resistance in the heart. Biomol. Ther. (Seoul) 25, 44-56.   DOI
10 O'Hara, D. S. and Lefkowitz, R. J. (1974) Affinity chromatography of adrenergic receptors and binding proteins. Meth. Enzymol. 34, 695-700.
11 Park, S. J. and Im, D. S. (2017) Sphingosine 1-phosphate receptor modulators and drug discovery. Biomol. Ther. (Seoul) 25, 80-90.   DOI
12 Reiter, E., Ahn, S., Shukla, A. K. and Lefkowitz, R. J. (2012) Molecular mechanism of ${\beta}$-arrestin-biased agonism at seven-transmembrane receptors. Annu. Rev. Pharmacol. Toxicol. 52, 179-197.   DOI
13 van Biesen, T., Hawes, B. E., Luttrell, D. K., Krueger, K. M., Touhara, K., Porfiri, E., Sakaue, M., Luttrell, L. M. and Lefkowitz, R. J. (1995) Receptor-tyrosine-kinase- and $G{\beta}{\gamma}$-mediated MAP kinase activation by a common signalling pathway. Nature 376, 781-784.   DOI
14 Robison, G. A., Butcher, R. W. and Sutherland, E. W. (1967) Adenyl cyclase as an adrenergic receptor. Ann. N. Y. Acad. Sci. 139, 703-723.   DOI
15 Rodbell, M., Birnbaumer, L., Pohl, S. L. and Krans, H. M. (1971) The glucagon-sensitive adenyl cyclase system in plasma membranes of rat liver. V. An obligatory role of guanylnucleotides in glucagon action. J. Biol. Chem. 246, 1877-1882.
16 Rosenbaum, D. M., Cherezov, V., Hanson, M. A., Rasmussen, S. G., Thian, F. S., Kobilka, T. S., Choi, H. J., Yao, X. J., Weis, W. I., Stevens, R. C. and Kobilka, B. K. (2007) GPCR engineering yields high-resolution structural insights into ${\beta}$2-adrenergic receptor function. Science 318, 1266-1273.   DOI
17 Sodhi, A., Montaner, S. and Gutkind, J. S. (2004) Viral hijacking of Gprotein-coupled-receptor signalling networks. Nat. Rev. Mol. Cell Biol. 5, 998-1012.   DOI
18 Stryer, L. (1986) Cyclic GMP cascade of vision. Annu. Rev. Neurosci. 9, 87-119.   DOI
19 Violin, J. D. and Lefkowitz, R. J. (2007) ${\beta}$-arrestin-biased ligands at seven-transmembrane receptors. Trends Pharmacol. Sci. 28, 416-422.   DOI
20 Wei, H., Ahn, S., Shenoy, S. K., Karnik, S. S., Hunyady, L., Luttrell, L. M. and Lefkowitz, R. J. (2003) Independent ${\beta}$-arrestin 2 and G protein-mediated pathways for angiotensin II activation of extracellular signal-regulated kinases 1 and 2. Proc. Natl. Acad. Sci. U.S.A. 100, 10782-10787.   DOI
21 Cherezov, V., Rosenbaum, D. M., Hanson, M. A., Rasmussen, S. G., Thian, F. S., Kobilka, T. S., Choi, H. J., Kuhn, P., Weis, W. I., Kobilka, B. K. and Stevens, R. C. (2007) High-resolution crystal structure of an engineered human ${\beta}2$-adrenergic G-protein-coupled receptor. Science 318, 1258-1265.   DOI
22 Bologna, Z., Teoh, J., Bayoumi, A. S., Tang, Y. and Kim, I. M. (2017) Biased G protein-coupled receptor signaling: new player in modulating physiology and pathology. Biomol. Ther. (Seoul) 25, 12-25.   DOI
23 Cassel, D. and Selinger, Z. (1976) Catecholamine-stimulated GTPase activity in turkey erythrocyte membranes. Biochim. Biophys. Acta 452, 538-551.   DOI
24 Chen, Y., Long, H., Wu, Z., Jiang, X. and Ma, L. (2008) EGF transregulates opioid receptors through EGFR-mediated GRK2 phosphorylation and activation. Mol. Biol. Cell 19, 2973-2983.   DOI
25 Chou, M. M., Hou, W., Johnson, J., Graham, L. K., Lee, M. H., Chen, C. S., Newton, A. C., Schaffhausen, B. S. and Toker, A. (1998) Regulation of protein kinase C zeta by PI 3-kinase and PDK-1. Curr. Biol. 8, 1069-1077.   DOI
26 Daub, H., Weiss, F. .U, Wallasch, C. and Ullrich, A. (1996) Role of transactivation of the EGF receptor in signalling by G-protein-coupled receptors. Nature 379, 557-560.   DOI
27 Dixon, R. A., Kobilka, B. K., Strader, D. J., Benovic, J. L., Dohlman, H. G., Frielle, T., Bolanowski, M. A., Bennett, C. D., Rands, E., Diehl, R. E., Mumford, R. A., Slater, E. E., Sigal, I. S., Caron, M. G., Lefkowitz, R. J. and Strader, C. D. (1986) Cloning of the gene and cDNA for mammalian ${\beta}$-adrenergic receptor and homology with rhodopsin. Nature 321, 75-79.   DOI
28 Duc, N. M., Kim, H. R. and K. Y. Chung (2017) Recent progress in understanding the conformational mechanism of heterotrimeric G protein activation. Biomol. Ther. (Seoul) 25, 4-11.   DOI
29 Whalen, E. J., Rajagopal, S. and Lefkowitz, R. J. (2011) Therapeutic potential of ${\beta}$-arrestin- and G protein-biased agonists. Trends Mol. Med. 17, 126-139.   DOI
30 Weichert, D., Banerjee, A., Hiller, C., Kling, R. C., Hubner, H. and Gmeiner, P. (2015) Molecular determinants of biased agonism at the dopamine $D_2$ receptor. J. Med. Chem. 58, 2703-2717.   DOI
31 Zhang, X. and Kim, K. M. (2017) Multifactorial regulation of G proteincoupled receptor endocytosis. Biomol. Ther. (Seoul) 25, 26-43.   DOI
32 Zheng, M., Zhang, X., Guo, S., Zhang, X., Min, C., Cheon, S. H., Oak, M. H., Kim, Y. R. and Kim, K. M. (2016) Agonist-induced changes in RalA activities allows the prediction of the endocytosis of G proteincoupled receptors. Biochim. Biophys. Acta 1863, 77-90.   DOI