{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,15]],"date-time":"2026-10-15T19:39:06Z","timestamp":1792093146815,"version":"4.4.0"},"reference-count":81,"publisher":"Wiley","issue":"12","license":[{"start":{"date-parts":[[2024,5,17]],"date-time":"2024-05-17T00:00:00Z","timestamp":1715904000000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by-nc-nd\/4.0\/"}],"funder":[{"DOI":"10.13039\/100013349","name":"LABoratoires d\u2019EXcellence ARCANE","doi-asserted-by":"publisher","id":[{"id":"10.13039\/100013349","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["chemistry-europe.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["ChemBioChem"],"published-print":{"date-parts":[[2024,6,17]]},"abstract":"<jats:title>Abstract<\/jats:title>\n                  <jats:p>G\u2010quadruplex DNA structures (G4) are proven to interfere with most genetic and epigenetic processes. Small molecules binding these structures (G4 ligands) are invaluable tools to probe G4\u2010biology and address G4\u2010druggability in various diseases (cancer, viral infections). However, the large number of reported G4 ligands (&gt;1000) could lead to confusion while selecting one for a given application. Herein we conducted a systematic affinity ranking of 11\u2005popular G4 ligands vs 5\u2005classical G4 sequences using FRET\u2010melting, G4\u2010FID assays and SPR. Interestingly SPR data globally align with the rankings obtained from the two semi\u2010quantitative assays despite discrepancies due to limits and characteristics of each assay. In the whole, PhenDC3 emerges as the most potent binder irrespective of the G4 sequence. Immediately below PDS, PDC\u2010360A, BRACO19, TMPyP4 and RHPS4 feature strong to medium binding again with poor G4 topology discrimination. More strikingly, the G4 drugs Quarfloxin, CX5461 and c\u2010PDS exhibit weak affinity with all G4s studied. Finally, NMM and Cu\u2010ttpy showed heterogeneous behaviors due, in part, to their physicochemical particularities poorly compatible with screening conditions. The remarkable properties of PhenDC3 led us to propose its use for benchmarking FRET\u2010melting and G4\u2010FID assays for rapid G4\u2010affinity evaluation of newly developed ligands.<\/jats:p>","DOI":"10.1002\/cbic.202400210","type":"journal-article","created":{"date-parts":[[2024,4,15]],"date-time":"2024-04-15T12:38:47Z","timestamp":1713184727000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":10,"title":["Systematic Evaluation of Benchmark G4 Probes and G4 Clinical Drugs using three Biophysical Methods: A Guideline to Evaluate Rapidly G4\u2010Binding Affinity"],"prefix":"10.1002","volume":"25","author":[{"given":"E.","family":"Laigre","sequence":"first","affiliation":[{"name":"CNRS UMR9187 INSERM U1196 Institut Curie PSL Research University  F-91405 Orsay France"},{"name":"CNRS UMR9187 INSERM U1196 Universit\u00e9 Paris-Saclay  F-91405 Orsay France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"H.","family":"Bonnet","sequence":"additional","affiliation":[{"name":"DCM UMR 5250 Univ. Grenoble Alpes CNRS  570 Rue de la Chimie 38000 Grenoble France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"C.","family":"Beauvineau","sequence":"additional","affiliation":[{"name":"CNRS UMR9187 INSERM U1196 Institut Curie PSL Research University  F-91405 Orsay France"},{"name":"CNRS UMR9187 INSERM U1196 Universit\u00e9 Paris-Saclay  F-91405 Orsay France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-0029-0015","authenticated-orcid":false,"given":"T.","family":"Lavergne","sequence":"additional","affiliation":[{"name":"DCM UMR 5250 Univ. Grenoble Alpes CNRS  570 Rue de la Chimie 38000 Grenoble France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7555-6033","authenticated-orcid":false,"given":"D.","family":"Verga","sequence":"additional","affiliation":[{"name":"CNRS UMR9187 INSERM U1196 Institut Curie PSL Research University  F-91405 Orsay France"},{"name":"CNRS UMR9187 INSERM U1196 Universit\u00e9 Paris-Saclay  F-91405 Orsay France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3911-6241","authenticated-orcid":false,"given":"E.","family":"Defrancq","sequence":"additional","affiliation":[{"name":"DCM UMR 5250 Univ. Grenoble Alpes CNRS  570 Rue de la Chimie 38000 Grenoble France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2434-2959","authenticated-orcid":false,"given":"J.","family":"Dejeu","sequence":"additional","affiliation":[{"name":"DCM UMR 5250 Univ. Grenoble Alpes CNRS  570 Rue de la Chimie 38000 Grenoble France"},{"name":"SUPMICROTECH Universit\u00e9 Franche-Comt\u00e9 CNRS Institut FEMTO-ST  25000 Besan\u00e7on France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2053-7513","authenticated-orcid":false,"given":"M.\u2010P.","family":"Teulade\u2010Fichou","sequence":"additional","affiliation":[{"name":"CNRS UMR9187 INSERM U1196 Institut Curie PSL Research University  F-91405 Orsay France"},{"name":"CNRS UMR9187 INSERM U1196 Universit\u00e9 Paris-Saclay  F-91405 Orsay France"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2024,5,17]]},"reference":[{"key":"e_1_2_10_1_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.tig.2022.11.005"},{"key":"e_1_2_10_2_1","doi-asserted-by":"publisher","DOI":"10.1002\/mc.20507"},{"key":"e_1_2_10_3_1","doi-asserted-by":"publisher","DOI":"10.1039\/c1cs15153c"},{"key":"e_1_2_10_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.tcb.2009.05.002"},{"key":"e_1_2_10_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.jmb.2013.09.026"},{"key":"e_1_2_10_6_1","doi-asserted-by":"publisher","DOI":"10.1093\/nar\/gkab609"},{"key":"e_1_2_10_7_1","doi-asserted-by":"publisher","DOI":"10.15252\/embj.201490702"},{"key":"e_1_2_10_8_1","doi-asserted-by":"publisher","DOI":"10.1093\/nar\/gkv193"},{"key":"e_1_2_10_9_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41467-019-11104-0"},{"key":"e_1_2_10_10_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41580-020-0236-x"},{"key":"e_1_2_10_11_1","doi-asserted-by":"publisher","DOI":"10.1093\/nar\/gkab187"},{"key":"e_1_2_10_12_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.tibs.2020.11.001"},{"key":"e_1_2_10_13_1","doi-asserted-by":"publisher","DOI":"10.1159\/000516394"},{"key":"e_1_2_10_14_1","doi-asserted-by":"publisher","DOI":"10.1038\/nchem.1548"},{"key":"e_1_2_10_15_1","doi-asserted-by":"publisher","DOI":"10.1021\/acschembio.9b00934"},{"key":"e_1_2_10_16_1","doi-asserted-by":"publisher","DOI":"10.1093\/nar\/gkab1166"},{"key":"e_1_2_10_17_1","doi-asserted-by":"publisher","DOI":"10.1093\/nar\/gkq136"},{"key":"e_1_2_10_18_1","doi-asserted-by":"publisher","DOI":"10.1074\/jbc.M113.496463"},{"key":"e_1_2_10_19_1","doi-asserted-by":"publisher","DOI":"10.7554\/eLife.46793"},{"key":"e_1_2_10_20_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.trechm.2019.07.002"},{"key":"e_1_2_10_21_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.biochem.9b01094"},{"key":"e_1_2_10_22_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2019.05.042"},{"key":"e_1_2_10_23_1","doi-asserted-by":"publisher","DOI":"10.1093\/nar\/gkac915"},{"key":"e_1_2_10_24_1","doi-asserted-by":"publisher","DOI":"10.1038\/nchembio.780"},{"key":"e_1_2_10_25_1","doi-asserted-by":"publisher","DOI":"10.1002\/anie.201307413"},{"key":"e_1_2_10_26_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41467-018-07224-8"},{"key":"e_1_2_10_27_1","doi-asserted-by":"publisher","DOI":"10.1093\/nar\/gkz215"},{"key":"e_1_2_10_28_1","doi-asserted-by":"publisher","DOI":"10.1038\/ng.3662"},{"key":"e_1_2_10_29_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41570-017-0041"},{"key":"e_1_2_10_30_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.0c01145"},{"key":"e_1_2_10_31_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41467-021-24198-2"},{"key":"e_1_2_10_32_1","doi-asserted-by":"publisher","DOI":"10.1093\/nar\/gkab571"},{"key":"e_1_2_10_33_1","doi-asserted-by":"publisher","DOI":"10.1038\/ncomms16043"},{"key":"e_1_2_10_34_1","doi-asserted-by":"publisher","DOI":"10.1002\/anie.200906363"},{"key":"e_1_2_10_35_1","first-page":"243","volume-title":"Annu. Rep. Med. Chem., Vol. 54","author":"Granzhan A.","year":"2020"},{"key":"e_1_2_10_36_1","first-page":"1","volume-title":"Handbook of Chemical Biology of Nucleic Acids","author":"Verga D.","year":"2022"},{"key":"e_1_2_10_37_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.molcel.2015.12.004"},{"key":"e_1_2_10_38_1","doi-asserted-by":"publisher","DOI":"10.1038\/emboj.2011.316"},{"key":"e_1_2_10_39_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41467-021-27719-1"},{"key":"e_1_2_10_40_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.biochi.2015.06.002"},{"key":"e_1_2_10_41_1","doi-asserted-by":"publisher","DOI":"10.1007\/s00216-011-5018-z"},{"key":"e_1_2_10_42_1","doi-asserted-by":"publisher","DOI":"10.1007\/978-1-4939-9666-7_8"},{"key":"e_1_2_10_43_1","doi-asserted-by":"publisher","DOI":"10.1007\/978-1-4939-9666-7_3"},{"key":"e_1_2_10_44_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bbagen.2017.01.010"},{"key":"e_1_2_10_45_1","doi-asserted-by":"publisher","DOI":"10.3390\/ph14080769"},{"key":"e_1_2_10_46_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.5b01835"},{"key":"e_1_2_10_47_1","doi-asserted-by":"publisher","DOI":"10.1089\/154545703322860825"},{"key":"e_1_2_10_48_1","doi-asserted-by":"publisher","DOI":"10.1039\/C0CS00062K"},{"key":"e_1_2_10_49_1","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.081560598"},{"key":"e_1_2_10_50_1","doi-asserted-by":"publisher","DOI":"10.1186\/s13046-014-0081-x"},{"key":"e_1_2_10_51_1","first-page":"10376","volume":"43","author":"Bon\u010dina M.","year":"2015","journal-title":"Nucleic Acids Res."},{"key":"e_1_2_10_52_1","doi-asserted-by":"publisher","DOI":"10.1039\/C9CP06321H"},{"key":"e_1_2_10_53_1","doi-asserted-by":"publisher","DOI":"10.1002\/chem.201700417"},{"key":"e_1_2_10_54_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bpc.2006.06.006"},{"key":"e_1_2_10_55_1","doi-asserted-by":"publisher","DOI":"10.1158\/0008-5472.CAN-09-1304"},{"key":"e_1_2_10_56_1","doi-asserted-by":"publisher","DOI":"10.1038\/ncomms14432"},{"key":"e_1_2_10_57_1","doi-asserted-by":"publisher","DOI":"10.1002\/anie.201206281"},{"key":"e_1_2_10_58_1","doi-asserted-by":"publisher","DOI":"10.1093\/nar\/gku1274"},{"key":"e_1_2_10_59_1","doi-asserted-by":"publisher","DOI":"10.1093\/nar\/gkp630"},{"key":"e_1_2_10_60_1","doi-asserted-by":"publisher","DOI":"10.1021\/ja208993r"},{"key":"e_1_2_10_61_1","doi-asserted-by":"publisher","DOI":"10.1021\/ja501500c"},{"key":"e_1_2_10_62_1","doi-asserted-by":"publisher","DOI":"10.1021\/ja067352b"},{"key":"e_1_2_10_63_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bbrc.2004.08.150"},{"key":"e_1_2_10_64_1","doi-asserted-by":"publisher","DOI":"10.1039\/b708635k"},{"key":"e_1_2_10_65_1","doi-asserted-by":"publisher","DOI":"10.1039\/C4CC09744K"},{"key":"e_1_2_10_66_1","doi-asserted-by":"publisher","DOI":"10.3389\/fchem.2018.00281"},{"key":"e_1_2_10_67_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.langmuir.8b02942"},{"key":"e_1_2_10_68_1","doi-asserted-by":"publisher","DOI":"10.1002\/chem.201702076"},{"key":"e_1_2_10_69_1","doi-asserted-by":"publisher","DOI":"10.1002\/cmdc.201600171"},{"key":"e_1_2_10_70_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jpcc.8b07298"},{"key":"e_1_2_10_71_1","doi-asserted-by":"publisher","DOI":"10.1006\/abio.2000.4726"},{"key":"e_1_2_10_72_1","doi-asserted-by":"publisher","DOI":"10.1111\/febs.12734"},{"key":"e_1_2_10_73_1","doi-asserted-by":"publisher","DOI":"10.1093\/nar\/gks152"},{"key":"e_1_2_10_74_1","doi-asserted-by":"publisher","DOI":"10.1002\/chem.201601937"},{"key":"e_1_2_10_75_1","doi-asserted-by":"publisher","DOI":"10.1039\/c3cc44569k"},{"key":"e_1_2_10_76_1","doi-asserted-by":"publisher","DOI":"10.1002\/anie.201308063"},{"key":"e_1_2_10_77_1","doi-asserted-by":"publisher","DOI":"10.1021\/jacs.2c04775"},{"key":"e_1_2_10_78_1","doi-asserted-by":"publisher","DOI":"10.1002\/chem.201904923"},{"key":"e_1_2_10_79_1","doi-asserted-by":"publisher","DOI":"10.1002\/anie.202207384"},{"key":"e_1_2_10_80_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ymeth.2014.05.009"},{"key":"e_1_2_10_81_1","doi-asserted-by":"publisher","DOI":"10.1002\/chem.200903456"}],"container-title":["ChemBioChem"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/chemistry-europe.onlinelibrary.wiley.com\/doi\/pdf\/10.1002\/cbic.202400210","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,10,12]],"date-time":"2025-10-12T18:32:48Z","timestamp":1760293968000},"score":1,"resource":{"primary":{"URL":"https:\/\/chemistry-europe.onlinelibrary.wiley.com\/doi\/10.1002\/cbic.202400210"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2024,5,17]]},"references-count":81,"journal-issue":{"issue":"12","published-print":{"date-parts":[[2024,6,17]]}},"alternative-id":["10.1002\/cbic.202400210"],"URL":"https:\/\/doi.org\/10.1002\/cbic.202400210","archive":["Portico"],"relation":{},"ISSN":["1439-4227","1439-7633"],"issn-type":[{"value":"1439-4227","type":"print"},{"value":"1439-7633","type":"electronic"}],"subject":[],"published":{"date-parts":[[2024,5,17]]},"assertion":[{"value":"2024-04-08","order":0,"name":"received","label":"Received","group":{"name":"publication_history","label":"Publication History"}},{"value":"2024-05-17","order":3,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}],"article-number":"e202400210"}}