Please use this identifier to cite or link to this item: http://hdl.handle.net/1942/44879
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dc.contributor.authorHerman, Jean-
dc.contributor.authorVanstreels, Els-
dc.contributor.authorBardiot, Dorothee-
dc.contributor.authorProta, Andrea E.-
dc.contributor.authorGaillard, Natacha-
dc.contributor.authorGao, Ling-Jie-
dc.contributor.authorVercruysse, Thomas-
dc.contributor.authorPersoons, Leentje-
dc.contributor.authorDaems, Tinne-
dc.contributor.authorWaer , Mark-
dc.contributor.authorHerdewijn, Piet-
dc.contributor.authorLouat, Thierry-
dc.contributor.authorSteinmetz, Michel O.-
dc.contributor.authorDe Jonghe, Steven-
dc.contributor.authorSPRANGERS, Ben-
dc.contributor.authorDaelemans, Dirk-
dc.contributor.editorFaisal, Amir-
dc.date.accessioned2024-12-19T10:20:41Z-
dc.date.available2024-12-19T10:20:41Z-
dc.date.issued2024-
dc.date.submitted2024-12-17T11:09:23Z-
dc.identifier.citationPlos One, 19 (11) (Art N° e0307153)-
dc.identifier.urihttp://hdl.handle.net/1942/44879-
dc.description.abstractMicrotubule-targeting agents are an important class of anti-cancer drugs; their full potential is however not realized because of significant myelotoxicity and neurotoxicity. We here report 3-nitropyridine analogues as a novel group of microtubule-targeting agents with potent anti-cancer effects against a broad range of cancer types. We show that these 3-nitropyridines induce cell cycle arrest in the G2-M phase and inhibit tubulin polymerization by interacting with tubulin. Determination of the tubulin-4AZA2996 structure by X-ray crystallography demonstrated that this class of compounds binds to the colchicine-site of tubulin. Furthermore, the anti-cancer effect was demonstrated both in vitro and in vivo in a murine heterotopic xenograft model of colon cancer. When administered intravenously, 4AZA2891 effectively inhibited cancer growth. Whereas 3-nitropyridine compounds do not induce myelotoxicity at pharmacological doses, the neurotoxicity associated with microtubule-targeting agents is still present.-
dc.description.sponsorshipThis research was supported by grant 31003A_166608 from the Swiss National Science Fou dation (https://www.snf.ch/en) to MOS. BS is senior clinical investigator of the Research Foundation Flanders (FWO, 1842919N, https:// www.fwo.be/).The funders did not play any role in the study design, data collection and analysis, decision to publish, or preparation of the manuscript. We thank the staff of beamline X06DA of the Swiss Light Source (Paul Scherrer Institut, Villigen PSI, Switzerland) and the KU Leuven technical staff involved in laboratory experiments for their support.-
dc.language.isoen-
dc.publisherPUBLIC LIBRARY SCIENCE-
dc.rights2024 Herman et al. This is an open access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.-
dc.subject.otherAnimals-
dc.subject.otherHumans-
dc.subject.otherMice-
dc.subject.otherCell Line, Tumor-
dc.subject.otherTubulin Modulators-
dc.subject.otherCrystallography, X-Ray-
dc.subject.otherXenograft Model Antitumor Assays-
dc.subject.otherCell Proliferation-
dc.subject.otherMicrotubules-
dc.subject.otherTubulin-
dc.subject.otherPyridines-
dc.subject.otherAntineoplastic Agents-
dc.title3-nitropyridine analogues as novel microtubule-targeting agents-
dc.typeJournal Contribution-
dc.identifier.issue11-
dc.identifier.volume19-
local.format.pages16-
local.bibliographicCitation.jcatA1-
dc.description.notesDaelemans, D (corresponding author), Katholieke Univ Leuven, Dept Microbiol Immunol & Transplantat, Mol Genet & Therapeut Virol & Oncol Res Grp, Rega Inst, Leuven, Belgium.-
dc.description.notesdirk.daelemans@kuleuven.be-
local.publisher.place1160 BATTERY STREET, STE 100, SAN FRANCISCO, CA 94111 USA-
local.type.refereedRefereed-
local.type.specifiedArticle-
local.bibliographicCitation.artnre0307153-
dc.identifier.doi10.1371/journal.pone.0307153-
dc.identifier.pmid39509402-
dc.identifier.isiWOS:001364384500004-
dc.contributor.orcidProta, Andrea E./0000-0003-0875-5339-
dc.identifier.eissn-
local.provider.typewosris-
local.description.affiliation[Herman, Jean; Bardiot, Dorothee; Gao, Ling-Jie; Daems, Tinne; Waer, Mark; Herdewijn, Piet; Louat, Thierry; De Jonghe, Steven] 4AZA Biosci, Leuven, Belgium.-
local.description.affiliation[Herman, Jean; Gao, Ling-Jie; Waer, Mark; Herdewijn, Piet; Louat, Thierry; De Jonghe, Steven; Sprangers, Ben] Katholieke Univ Leuven, Interface Valorisat Platform IVAP, Leuven, Belgium.-
local.description.affiliation[Herman, Jean; Waer, Mark; Sprangers, Ben] Katholieke Univ Leuven, Dept Microbiol Immunol & Transplantat, Lab Mol Immunol, Rega Inst, Leuven, Belgium.-
local.description.affiliation[Herman, Jean] Univ Hosp Leuven, Dept Pediat Nephrol & Solid Organ Transplantat, Leuven, Belgium.-
local.description.affiliation[Vanstreels, Els; Vercruysse, Thomas; Persoons, Leentje; Daelemans, Dirk] Katholieke Univ Leuven, Dept Microbiol Immunol & Transplantat, Mol Genet & Therapeut Virol & Oncol Res Grp, Rega Inst, Leuven, Belgium.-
local.description.affiliation[Prota, Andrea E.; Gaillard, Natacha; Steinmetz, Michel O.] Paul Scherrer Inst, Ctr Life Sci, Lab Biomol Res, Wurenlingen, Switzerland.-
local.description.affiliation[Gao, Ling-Jie; Herdewijn, Piet] Katholieke Univ Leuven, Dept Pharmaceut & Pharmacol Sci, Med Chem Lab, Rega Inst, Leuven, Belgium.-
local.description.affiliation[Steinmetz, Michel O.] Univ Basel, Basel, Switzerland.-
local.description.affiliation[De Jonghe, Steven] Katholieke Univ Leuven, Dept Microbiol Immunol & Transplantat, Mol Struct & Translat Virol Res Grp, Rega Inst, Leuven, Belgium.-
local.description.affiliation[Sprangers, Ben] Univ Hosp Leuven, Dept Nephrol, Leuven, Belgium.-
local.description.affiliation[Bardiot, Dorothee] CISTIM Leuven Vzw, Leuven, Belgium.-
local.description.affiliation[Daems, Tinne] Aminolabs, Hasselt Res Campus 6, Hasselt, Belgium.-
local.uhasselt.internationalyes-
item.fulltextWith Fulltext-
item.contributorHerman, Jean-
item.contributorVanstreels, Els-
item.contributorBardiot, Dorothee-
item.contributorProta, Andrea E.-
item.contributorGaillard, Natacha-
item.contributorGao, Ling-Jie-
item.contributorVercruysse, Thomas-
item.contributorPersoons, Leentje-
item.contributorDaems, Tinne-
item.contributorWaer , Mark-
item.contributorHerdewijn, Piet-
item.contributorLouat, Thierry-
item.contributorSteinmetz, Michel O.-
item.contributorDe Jonghe, Steven-
item.contributorSPRANGERS, Ben-
item.contributorDaelemans, Dirk-
item.contributorFaisal, Amir-
item.fullcitationHerman, Jean; Vanstreels, Els; Bardiot, Dorothee; Prota, Andrea E.; Gaillard, Natacha; Gao, Ling-Jie; Vercruysse, Thomas; Persoons, Leentje; Daems, Tinne; Waer , Mark; Herdewijn, Piet; Louat, Thierry; Steinmetz, Michel O.; De Jonghe, Steven; SPRANGERS, Ben & Daelemans, Dirk (2024) 3-nitropyridine analogues as novel microtubule-targeting agents. In: Plos One, 19 (11) (Art N° e0307153).-
item.accessRightsOpen Access-
crisitem.journal.issn1932-6203-
crisitem.journal.eissn1932-6203-
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