Generating thermostabilized agonist-bound GPR40/FFAR1 using virus-like particles and a label-free binding assay

References

• Araki T, Hirayama M, Hiroi S, Kaku K. 2012. GPR40-induced insulin secretion by the novel agonist TAK-875: first clinical findings in patients with type 2 diabetes. Diabetes Obes Metab 14:271–278
   PubMed Web of Science ®Google Scholar
• Bertheleme N, Singh S, Dowell SJ, Hubbard J, Byrne B. 2013. Loss of constitutive activity is correlated with increased thermostability of the human adenosine A2A receptor. Br J Pharmacol 169:988–998
   Google Scholar
• Burant CF, Viswanathan P, Marcinak J, Cao C, Vakilynejad M, Xie B, Leifke E. 2012. TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: A phase 2, randomised, double-blind, placebo-controlled trial. Lancet 379:1403–1411
   PubMed Web of Science ®Google Scholar
• Cherezov V, Rosenbaum DM, Hanson MA, Rasmussen SG, Thian FS, Kobilka TS, et al. 2007. High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor. Science 318:1258–1265
   PubMed Web of Science ®Google Scholar
• Chun E, Thompson AA, Liu W, Roth CB, Griffith MT, Katritch V, et al. 2012. Fusion partner toolchest for the stabilization and crystallization of G protein-coupled receptors. Structure 20:967–976
   Google Scholar
• Congreve M, Andrews SP, Dore AS, Hollenstein K, Hurrell E, Langmead CJ, et al. 2012. Discovery of 1,2,4-triazine derivatives as adenosine A(2A) antagonists using structure based drug design. J Med Chem 55:1898–1903
   PubMed Web of Science ®Google Scholar
• Congreve M, Langmead C, Marshall FH. 2011a. The use of GPCR structures in drug design. Adv Pharmacol 62:1–36
   Google Scholar
• Congreve M, Rich RL, Myszka DG, Figaroa F, Siegal G, Marshall FH. 2011b. Fragment screening of stabilized G-protein-coupled receptors using biophysical methods. Methods Enzymol 493:115–136
   PubMed Web of Science ®Google Scholar
• Dore AS, Robertson N, Errey JC, Ng I, Hollenstein K, Tehan B, et al. 2011. Structure of the adenosine A(2A) receptor in complex with ZM241385 and the xanthines XAC and caffeine. Structure 19:1283–1293
   PubMed Web of Science ®Google Scholar
• Itoh Y, Kawamata Y, Harada M, Kobayashi M, Fujii R, Fukusumi S, et al. 2003. Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40. Nature 422:173–176
   PubMed Web of Science ®Google Scholar
• Kobilka BK, Deupi X. 2007. Conformational complexity of G-protein-coupled receptors. Trends Pharmacol Sci 28:397–406
   PubMed Web of Science ®Google Scholar
• Kolb P, Rosenbaum DM, Irwin JJ, Fung JJ, Kobilka BK, Shoichet BK. 2009. Structure-based discovery of beta2-adrenergic receptor ligands. Proc Natl Acad Sci USA 106:6843–6848
   PubMed Web of Science ®Google Scholar
• Lagerstrom MC, Schioth HB. 2008. Structural diversity of G protein-coupled receptors and significance for drug discovery. Nat Rev Drug Discov 7:339–357
   PubMed Web of Science ®Google Scholar
• Lebon G, Bennett K, Jazayeri A, Tate CG. 2011. Thermostabilisation of an agonist-bound conformation of the human adenosine A(2A) receptor. J Mol Biol 409:298–310
   PubMed Web of Science ®Google Scholar
• Leifke E, Naik H, Wu J, Viswanathan P, Demanno D, Kipnes M, Vakilynejad M. 2012. A multiple-ascending-dose study to evaluate safety, pharmacokinetics, and pharmacodynamics of a novel GPR40 agonist, TAK-875, in subjects with type 2 diabetes. Clin Pharmacol Ther 92:29–39
   PubMed Web of Science ®Google Scholar
• Magnani F, Shibata Y, Serrano-Vega MJ, Tate CG. 2008. Co-evolving stability and conformational homogeneity of the human adenosine A2a receptor. Proc Natl Acad Sci USA 105:10744–10749
   PubMed Web of Science ®Google Scholar
• Miller JL, Tate CG. 2011. Engineering an ultra-thermostable beta(1)-adrenoceptor. J Mol Biol 413:628–638
   Google Scholar
• Muckenschnabel I, Falchetto R, Mayr LM, Filipuzzi I. 2004. SpeedScreen: Label-free liquid chromatography-mass spectrometry-based high-throughput screening for the discovery of orphan protein ligands. Anal Biochem 324:241–249
   PubMed Web of Science ®Google Scholar
• Naik H, Vakilynejad M, Wu J, Viswanathan P, Dote N, Higuchi T, Leifke E. 2012. Safety, tolerability, pharmacokinetics, and pharmacodynamic properties of the GPR40 agonist TAK-875: Results from a double-blind, placebo-controlled single oral dose rising study in healthy volunteers. J Clin Pharmacol 52:1007–1016
   PubMed Web of Science ®Google Scholar
• Robertson N, Jazayeri A, Errey J, Baig A, Hurrell E, Zhukov A, et al. 2011. The properties of thermostabilised G protein-coupled receptors (StaRs) and their use in drug discovery. Neuropharmacology 60:36–44
   PubMed Web of Science ®Google Scholar
• Serrano-Vega MJ, Magnani F, Shibata Y, Tate CG. 2008. Conformational thermostabilization of the beta1-adrenergic receptor in a detergent-resistant form. Proc Natl Acad Sci USA 105:877–882
   PubMed Web of Science ®Google Scholar
• Shibata Y, White JF, Serrano-Vega MJ, Magnani F, Aloia AL, Grisshammer R, Tate CG. 2009. Thermostabilization of the neurotensin receptor NTS1. J Mol Biol 390:262–277
   PubMed Web of Science ®Google Scholar
• Tate CG. 2012. A crystal clear solution for determining G-protein-coupled receptor structures. Trends Biochem Sci 37:343–352
   Google Scholar
• Tsujihata Y, Ito R, Suzuki M, Harada A, Negoro N, Yasuma T, et al. 2011. TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats. J Pharmacol Exp Ther 339:228–237
   PubMed Web of Science ®Google Scholar
• Ulrik G, Juan AB, Roland S, Elaine SB, Harel W, Brian KK. 1997. Structural instability of a constitutively active g protein-coupled receptor: agonist-independent activation due to conformational flexibility. J Biolog Chem 272:2587–2590
   Google Scholar
• Venkatakrishnan AJ, Deupi X, Lebon G, Tate CG, Schertler GF, Babu MM. 2013. Molecular signatures of G-protein-coupled receptors. Nature 494:185–194
   PubMed Web of Science ®Google Scholar
• Yabuki C, Komatsu H, Tsujihata Y, Maeda R, Ito R, Matsuda-Nagasumi K, et al. 2013. A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1. PLoS One 8:e76280
   PubMed Web of Science ®Google Scholar
• Yashiro H, Tsujihata Y, Takeuchi K, Hazama M, Johnson PR, Rorsman P. 2012. The effects of TAK-875, a selective G protein-coupled receptor 40/free fatty acid 1 agonist, on insulin and glucagon secretion in isolated rat and human islets. J Pharmacol Exp Ther 340:483–489
   PubMed Web of Science ®Google Scholar
• Zehender H, Le Goff F, Lehmann N, Filipuzzi I, Mayr LM. 2004. SpeedScreen: The ‘missing link’ between genomics and lead discovery. J Biomol Screen 9:498–505
   PubMed Web of Science ®Google Scholar
• Zhu B, Cai G, Hall E, Freeman G. 2007. In-Fusion™ assembly: Seamless engineering of multidomain fusion proteins, modular vectors, and mutations. BioTechniques 43:354–359
   PubMed Web of Science ®Google Scholar
• zur Megede J, Chen MC, Doe B, Schaefer M, Greer CE, Selby M, et al. 2000. Increased expression and immunogenicity of sequence-modified human immunodeficiency virus type 1 gag gene. J Virol 74:2628–2635
   PubMed Web of Science ®Google Scholar