Technology combination to address GPCR allosteric modulator drug-discovery pitfalls

Drug Discovery Today: Technologies

Volumn 10, Issue 2, 2013, Pages

  Schann, Stephan ^a   Bouvier, Michel ^b   Neuville, Pascal ^a  

^a Bioparc   (France)

^b INSTITUTE FOR RESEARCH IN IMMUNOLOGY AND CANCER   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

G PROTEIN COUPLED RECEPTOR;

ALLOSTERISM; BINDING ASSAY; BINDING SITE; BIOLUMINESCENCE RESONANCE ENERGY TRANSFER; BIOSENSOR; CONFORMATIONAL TRANSITION; ENERGY TRANSFER; FLUORESCENCE RESONANCE ENERGY TRANSFER; HIGH THROUGHPUT SCREENING; LIGAND BINDING; LUMINESCENCE; NONHUMAN; PREDICTIVE VALUE; PROTEIN PROTEIN INTERACTION; REVIEW; SECOND MESSENGER; SIGNAL TRANSDUCTION; THERAPY EFFECT;

ALLOSTERIC REGULATION; BIOSENSING TECHNIQUES; DRUG DISCOVERY; FLUORESCENCE RESONANCE ENERGY TRANSFER; LIGANDS; LUMINESCENT MEASUREMENTS; RECEPTORS, G-PROTEIN-COUPLED;

EID: 84879882111     PISSN: None     EISSN: 17406749     Source Type: Journal    
DOI: 10.1016/j.ddtec.2012.09.008     Document Type: Review

References (41)

1. J.P. Overington How many drug targets are there? Nat. Rev. Drug Discov. 5 2006 993 996
2. K. Leach Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology TiPS 28 2007 382 389
3. B.J. Melancon Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery J. Med. Chem. 55 2012 1445 1464
4. A. Christopoulos G-protein-coupled receptor allosterism: the promise and the problem(s) Biochem. Soc. Trans. 32 Pt 5 2004 873 877
5. W. Stallaert Ligand functional selectivity and quantitative pharmacology at G protein-coupled receptors Expert Opin. Drug Discov. 6 2011 811 825
6. S. Galandrin The evasive nature of drug efficacy: implications for drug discovery Trends Pharmacol. Sci. 28 2007 423 430
7. T. Kenakin Allosteric modulators: the new generation of receptor antagonist Mol. Interv. 4 2004 222 229
8. Z.G. Gao Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers Biochem. Pharmacol. 82 2011 658 668
9. D. Wootten Allosteric modulation of endogenous metabolites as an avenue for drug discovery Mol. Pharmacol. 82 2012 281 290
10. S. Schann Chemical switch of a metabotropic glutamate receptor 2 silent allosteric modulator into dual metabotropic glutamate receptor 2/3 negative/positive allosteric modulators J. Med. Chem. 53 2010 8775 8779
11. M.B. Azzi Beta-arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors Proc. Natl. Acad. Sci. U. S. A. 100 2003 11406 11411
12. S. Galandrin, and M. Bouvier Distinct signaling profiles of beta1 and beta2 adrenergic receptors ligands toward adenylyl cyclase and mitogen-activated protein kinase reveals the pluridimensionality of efficacy Mol. Pharmacol. 70 2006 1575 1584
13. S. Galandrin Conformational rearrangements and signaling cascades involved in ligand-biased mitogen-activated protein kinase signaling through the beta1-adrenergic receptor Mol. Pharmacol. 74 2008 162 172
14. B.K. Kobilka, and X. Deupi Conformational complexity of G-protein-coupled receptors Trends Pharmacol. Sci. 28 2007 397 406
15. E. Goupil A novel biased allosteric compound inhibitor of parturition selectively impedes the prostaglandin F2alpha-mediated Rho/ROCK signaling pathway J. Biol. Chem. 285 2010 25624 25636
16. J.D. Violin Selectively engaging β-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance J. Pharmacol. Exp. Ther. 335 2010 572 579
17. T.J. Woltering Synthesis and characterization of 8-ethynyl-1,3-dihydro- benzo[b][1,4]diazepin-2-one derivatives: new potent non-competitive metabotropic glutamate receptor 2/3 antagonists. Part 1 Bioorg. Med. Chem. Lett. 17 2007 6811 6815
18. M. Kalinichev Selective mGluR2 negative allosteric modulators reverse the scopolamine-induced memory deficit in the novel object recognition test 40th Annual Meeting Neuroscience, SfN San Diego, CA, USA 2010 651 715
19. L.T. May Allosteric modulation of G protein-coupled receptors Annu. Rev. Pharmacol. Toxicol. 47 2007 1 51
20. T.M. Bridges, and C.W. Lindsley G-protein-coupled receptors: from classical modes of modulation to allosteric mechanisms ACS Chem. Biol. 3 2008 530 541
21. N.T. Burford Strategies for the identification of allosteric modulators of G-protein-coupled receptors Biochem. Pharmacol. 81 2011 691 702
22. S.D. Pratt Identification and characterization of mGlu3 ligands using a high throughput FLIPR assay for detection of agonists, antagonists, and allosteric modulators Comb. Chem. High Throughput Screen. 14 2011 631 641
23. C. Koole Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: implication for drug screening Mol. Pharmacol. 78 2010 456 465
24. D. Wooten Modulation of the glucagon-like peptide-1 receptor signaling by naturally occurring and synthetic flavonoids J. Pharmacol. Exp. Ther. 336 2011 540 550
25. L. Alvarez-Jaimes In vitro pharmacological characterization of RXFP3 allosterism: an example of probe dependency PLoS One 7 2012 e30792
26. C.M. Niswender Context-dependent pharmacology exhibited by negative allosteric modulators of metabotropic glutamate receptor 7 Mol. Pharmacol. 77 2010 459 468
27. L.B. Knudsen Functional importance of GLP-1 receptor species and expression levels in cell line Regul. Pept. 175 2012 21 29
28. B. Ilien Fluorescence resonance energy transfer to probe human M1 muscarinic receptor structure and drug binding properties J. Neurochem. 85 2003 768 778
29. C. Tahtaoui On the use of nonfluorescent dye labeled ligands in FRET-based receptor binding studies J. Med. Chem. 48 2005 7847 7859
30. S. Schann Sounds of silence: innovative approach for identification of novel GPCR-modulator chemical entities Proceedings of the 238th American Chemical Society National Meeting, MEDI Washington, DC, USA 2009 432
31. K.W. Sloop Novel small molecule glucagon-like peptide-1 receptor agonists stimulates insulin secretion in rodents and from human islets Diabetes 59 2010 3099 3107
32. M.R. Wood 'Molecular switches' on mGluR allosteric ligands that modulate modes of pharmacology Biochemistry 50 2011 2403 2410
33. I.M. Kim Beta-bloquers alprenolol and carvedilol stimulate beta-arrestin-mediated EGFR transactivation Proc. Natl. Acad. Sci. U. S. A. 105 2008 14555 14560
34. T. Noma Beta-arrestin-mediated beta1-adrenergic receptor transactivation of the EGFR confers cardioprotection J. Clin. Invest. 117 2007 2445 2458
35. R.W. Walters Beta-arrestin1 mediates nicotinic acid-induced flushing, but not its antilipolytic effect, in mice J. Clin. Invest. 119 2009 1312 1321
36. C. Galés Real-time monitoring of receptor and G-protein interactions in living cells Nat. Methods 2 2005 177 184
37. C. Galés Probing the activation-promoted structural rearrangements in preassembled receptor-G protein complexes Nat. Struct. Mol. Biol. 13 2006 778 786
38. P.G. Charest Monitoring agonist-promoted conformational changes of beta-arrestin in living cells by intramolecular BRET EMBO Rep. 6 2004 334 340
39. B. Breton Multiplexing of multicolor bioluminescence resonance energy transfer Biophys. J. 99 2010 4037 4046
40. B. Breton Combining resonance energy transfer methods reveals a complex between the alpha2A-adrenergic receptor, Galphai1beta1gamma2, and GRK2 FASEB J. 24 2010 4733 4743
41. M. Leduc Functional selectivity of natural and synthetic prostaglandin EP4 receptor ligands J. Pharmacol. Exp. Ther. 331 2009 297 307