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dc.contributor.author | Gaugaz, Fabienne Z. | - |
dc.contributor.author | Chicca, Andrea | - |
dc.contributor.author | Redondo-Horcajo, Mariano | - |
dc.contributor.author | Barasoain, Isabel | - |
dc.contributor.author | Díaz, José Fernando | - |
dc.contributor.author | Altmann, Karl-Heinz | - |
dc.date.accessioned | 2019-03-15T13:54:38Z | - |
dc.date.available | 2019-03-15T13:54:38Z | - |
dc.date.issued | 2019-03-05 | - |
dc.identifier.citation | International Journal of Molecular Sciences 20(5): 1113 (2019) | - |
dc.identifier.issn | 1661-6596 | - |
dc.identifier.uri | http://hdl.handle.net/10261/178031 | - |
dc.description.abstract | A new simplified, epoxide-free epothilone analog was prepared incorporating an N-(2-hydroxyethyl)-benzimidazole side chain, which binds to microtubules with high affinity and inhibits cancer cell growth in vitro with nM potency. Building on this scaffold, a disulfide-linked conjugate with the purported EGFR-binding (EGFR, epidermal growth factor receptor) peptide GE11 was then prepared. The conjugate retained significant microtubule-binding affinity, in spite of the size of the peptide attached to the benzimidazole side chain. The antiproliferative activity of the conjugate was significantly lower than for the parent scaffold and, surprisingly, was independent of the EGFR expression status of cells. Our data indicate that the disulfide-based conjugation with the GE11 peptide is not a viable approach for effective tumor-targeting of highly potent epothilones and probably not for other cytotoxics. | - |
dc.description.sponsorship | We are indebted to the Swiss National Science Foundation (F.G.Z.; project number 205320-117594) and the ETH Zürich for generous financial support. This work was also supported by Ministerio de Economia y Competitividad grant BFU2016-75319-R to FDP (AEI/FEDER, UE). We thank Ganadería Fernando Díaz for the supply of calf brains. The authors acknowledge networking contributions by the COST Action CM1407 “Challenging organic syntheses inspired by nature - from natural products chemistry to drug discovery” and the COST action CM1470 | - |
dc.description.sponsorship | We acknowledge support by the CSIC Open Access Publication Initiative through its Unit of Information Resources for Research (URICI) | - |
dc.publisher | Multidisciplinary Digital Publishing Institute | - |
dc.relation | info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/BFU2016-75319-R | - |
dc.relation.isversionof | Publisher's version | - |
dc.rights | openAccess | - |
dc.subject | Cancer | - |
dc.subject | Drug discovery | - |
dc.subject | Epothilone | - |
dc.subject | Medicinal chemistry | - |
dc.subject | Microtubule-stabilizing agents | - |
dc.subject | Prodrug | - |
dc.subject | Total synthesis | - |
dc.subject | Tumor-targeting | - |
dc.title | Synthesis, Microtubule-Binding Affinity, and Antiproliferative Activity of New Epothilone Analogs and of an EGFR-Targeted Epothilone-Peptide Conjugate | - |
dc.type | artículo | - |
dc.identifier.doi | 10.3390/ijms20051113 | - |
dc.description.peerreviewed | Peer reviewed | - |
dc.relation.publisherversion | http://dx.doi.org/10.3390/ijms20051113 | - |
dc.identifier.e-issn | 1422-0067 | - |
dc.date.updated | 2019-03-15T13:54:39Z | - |
dc.rights.license | http://creativecommons.org/licenses/by-nc-sa/4.0/ | - |
dc.contributor.funder | Consejo Superior de Investigaciones Científicas (España) | - |
dc.contributor.funder | Swiss National Science Foundation | - |
dc.contributor.funder | Federal Institute of Technology Zurich | - |
dc.contributor.funder | Ministerio de Economía y Competitividad (España) | - |
dc.contributor.funder | European Commission | - |
dc.relation.csic | Sí | - |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003329 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003339 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003006 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100000780 | es_ES |
dc.identifier.pmid | 30841526 | - |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.cerifentitytype | Publications | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.grantfulltext | open | - |
item.openairetype | artículo | - |
item.fulltext | With Fulltext | - |
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ijms-20-01113.pdf | 1,44 MB | Adobe PDF | Visualizar/Abrir |
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