G-protein-coupled receptor-based drugs rediscovered

Future Medicinal ChemistryVol. 9, No. 7 EditorialG-protein-coupled receptor-based drugs rediscoveredKenneth LundstromKenneth Lundstrom*Author for correspondence: E-mail Address: lundstromkenneth@gmail.com PanTherapeutics, Lutry, SwitzerlandPublished Online:15 May 2017https://doi.org/10.4155/fmc-2017-0045AboutSectionsView ArticleView Full TextPDF/EPUB ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareShare onFacebookTwitterLinkedInReddit View articleKeywords: cell-based technologiesGPCR structuresvirtual screeningReferences1 Thompson MD, Burnham WM, Cole DE. The G-protein-coupled receptors: pharmacogenetics and disease. Crit. Rev. Clin. Lab. Sci. 42(4), 311–392 (2005).Crossref, Medline, CAS, Google Scholar2 Veljkovic V, Veljkovic N, Este J et al. Application of the EIIP/ISM bioinformatics concept in development of new drugs. Curr. Med. Chem. 14(4), 441–453 (2007).Crossref, Medline, CAS, Google Scholar3 Cherezov V, Rosenbaum DM, Hanson MA et al. High-resolution structure of an engineered human beta-2 adrenergic G-protein-coupled receptor. Science 318(5854), 1258–1265 (2007).Crossref, Medline, CAS, Google Scholar4 Zhang G, Wang K, Li XD et al. Discovery of novel antagonists of human neurotensin receptor 1 on the basis of ligand and protein structure. Biomed. Pharmacother. 84, 147–157 (2016).Crossref, Medline, CAS, Google Scholar5 Miao Y, Goldfeld DA, Moo EV et al. Accelerated structure-based design of chemically allosteric modulators of a muscarinic G-protein-coupled receptor. Proc. Natl Acad. Sci. USA 113(38), E5675–E5684 (2016).Crossref, Medline, CAS, Google Scholar6 Vass M, Kooistra Aj, Ritschel T et al. Molecular interaction fingerprint approaches for GPCRs. Curr. Opin. Pharmacol. 30, 59–68 (2016).Crossref, Medline, CAS, Google Scholar7 Bresso E, Togawa R, Hammond-Kosack K et al. GPCRs from Fusarium graminearum detection, modeling and virtual screening – the search for new routes to control head blight disease. BMC Bioinformatics 17(Suppl. 18), 463 (2016).Crossref, Medline, Google Scholar8 Lundstrom K. Present and future approaches to screening of G-protein-coupled receptors. Future Med. Chem. 5(5), 523–538 (2013).Link, CAS, Google Scholar9 Williams C. cAMP detection methods in HTS: selecting the best from the rest. Nat. Rev. Drug Discov. 3(2), 125–135 (2004).Crossref, Medline, CAS, Google Scholar10 Cheng Z, Garvin D, Paguio A et al. Luciferase reporter assay system for deciphering GPCR pathways. Curr. Chem. Genomics 4, 84–91 (2010).Crossref, Medline, CAS, Google Scholar11 Zhao CK, Yin Q, Li SY. A high throughput screening system for G-protein-coupled receptors using β-lactamase enzyme complementation technology. Acta Pharmacol. Sin. 31(12), 1618–1624 (2010).Crossref, Medline, CAS, Google Scholar12 van Der Lee MM, Bras M, van Koppen CJ et al. Beta-arrestin recruitment assay for identification of agonists for the sphingosine-1 phosphate receptor EDG1. J. Biomol. Screen. 13(10), 986–998 (2008).Crossref, Medline, CAS, Google Scholar13 Allen JA, Yost JM, Setola V et al. Discovery of β-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy. Proc. Natl Acad. Sci. USA 108(45), 18488–18493 (2011).Crossref, Medline, CAS, Google Scholar14 Yu N, Atienza JM, Bernard J et al. Real-time monitoring of morphological changes in living cells by electronic cell sensor arrays: an approach to study G-protein-coupled receptors. Anal. Chem. 78(1), 35–43 (2006).Crossref, Medline, CAS, Google Scholar15 Halai R, Cooper MA. Using label-free screening technology to improve efficiency in drug discovery. Expert Opin. Drug Discov. 7(2), 123–131 (2012).Crossref, Medline, CAS, Google Scholar16 Solly K, Wang X, Xu X et al. Application of real-time cell electronic sensing (RT-CES) technology to cell-based assays. Assay Drug Dev. Technol. 2(4), 363–372 (2004).Crossref, Medline, CAS, Google Scholar17 Thomsen W, Frazer J, Unett D. Functional assays for screening GPCR targets. Curr. Opin. Biotechnol. 16(6), 655–665 (2005).Medline, CAS, Google Scholar18 Lee PH. Label-free optical biosensor: a tool for G-protein-coupled receptors pharmacology profiling and inverse agonists identification. J. Recept. Signal Transd. Res. 29(3–4), 146–153 (2009).Crossref, Medline, CAS, Google Scholar19 An WF, Tolliday N. Cell-based assays for high-throughput screening. Mol. Biotechnol. 45(2), 180–186 (2010).Crossref, Medline, CAS, Google Scholar20 McGuinness RP, Proctor JM, Gallant DL et al. Enhanced selectivity screening of GPCR ligands using a label-free cell based assay technology. Comb. Chem. High Throughput Screen. 12(8), 812–823 (2009).Crossref, Medline, CAS, Google Scholar21 Peters MF, Vaillancourt F, Heroux M et al. Comparing label-free biosensors for pharmacological screening with cell-based functional assays. Assay Drug Dev. Technol. 8(2), 219–227 (2010).Crossref, Medline, CAS, Google Scholar22 ACEA Biosciences Inc. xCELLigence RTCA Systems. https://aceabio.com/products/xcelligence-rtca/Google Scholar23 Gonzalez-Maeso J. GPCR oligomers in pharmacology and signaling. Mol. Brain 4(1), 20 (2011).Crossref, Medline, CAS, Google Scholar24 Rozenfeld R, Gupta A, Gagnidze K et al. AT1R-CBR heteromerization reveals a new mechanism for the pathogenic properties of angiotensin II. EMBO J. 30(12), 2350–2363 (2011).Crossref, Medline, CAS, Google Scholar25 Farran B. An update on the physiological and therapeutic relevance of GPCR oligomers. Pharmacol. Res. 117, 303–327 (2017).Crossref, Medline, CAS, Google Scholar26 Maurel D, Comps-Agrar L, Brock C et al. Cell-surface protein–protein interaction analysis with time-resolved FRET and snap-tag technologies: applications to G-protein-coupled receptor oligomerization. Methods Mol. Biol. 756, 201–214 (2011).Crossref, Medline, Google Scholar27 Kaczor AA, Selent J, Poso A. Structure-based molecular modeling approaches to GPCR oligomerization. Methods Cell Biol. 117, 91–104 (2013).Crossref, Medline, CAS, Google ScholarFiguresReferencesRelatedDetailsCited ByMPSM-DTI: prediction of drug–target interaction via machine learning based on the chemical structure and protein sequence1 January 2022 | Digital Discovery, Vol. 1, No. 2G-protein-coupled Receptors in Fungi19 June 2020Identification of a Conserved, Orphan G Protein-Coupled Receptor Required for Efficient Pathogen Clearance in Caenorhabditis elegansInfection and Immunity, Vol. 87, No. 4 Vol. 9, No. 7 Follow us on social media for the latest updates Metrics Downloaded 160 times History Published online 15 May 2017 Published in print May 2017 Information© Future Science LtdKeywordscell-based technologiesGPCR structuresvirtual screeningFinancial & competing interests disclosureThe author has no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.No writing assistance was utilized in the production of this manuscript.PDF download