Neutrophil Elastase-Activatable Prodrugs Based on an Alkoxyamine Platform to Deliver Alkyl Radicals Cytotoxic to Tumor Cells.
| dc.rights.license | open | en_US |
| hal.structure.identifier | Centre de résonance magnétique des systèmes biologiques [CRMSB] | |
| dc.contributor.author | SEREN, Seda | |
| dc.contributor.author | JOLY, Jean-Patrick | |
| hal.structure.identifier | Centre de résonance magnétique des systèmes biologiques [CRMSB] | |
| dc.contributor.author | VOISIN, Pierre | |
| hal.structure.identifier | Centre de résonance magnétique des systèmes biologiques [CRMSB] | |
| dc.contributor.author | BOUCHAUD, Véronique | |
| dc.contributor.author | AUDRAN, Gérard | |
| dc.contributor.author | MARQUE, Sylvain R A | |
| hal.structure.identifier | Centre de résonance magnétique des systèmes biologiques [CRMSB] | |
| dc.contributor.author | MELLET, Philippe | |
| dc.date.accessioned | 2022-11-30T15:56:29Z | |
| dc.date.available | 2022-11-30T15:56:29Z | |
| dc.date.issued | 2022-07-14 | |
| dc.identifier.issn | 1520-4804 | en_US |
| dc.identifier.uri | https://oskar-bordeaux.fr/handle/20.500.12278/170440 | |
| dc.description.abstractEn | Current chemotherapies suffer low specificity and sometimes drug resistance. Neutrophil elastase activity in cancer is associated with poor prognosis and metastasis settlement. More generally, tumors harbor various and persistent protease activities unseen in healthy tissues. In an attempt to be more specific, we designed prodrugs that are activatable by neutrophil elastase. Upon activation, these alkoxyamine-based drugs release cytotoxic alkyl radicals that act randomly to prevent drug resistance. As a result, U87 glioblastoma cells displayed high level caspase 3/7 activation during the first hour of exposure in the presence of human neutrophil elastase and the prodrug in vitro. The apoptosis process and cell death occurred between 24 and 48 h after exposure with a half lethal concentration of 150 μM. These prodrugs are versatile and easy to synthetize and can be adapted to many enzymes. | |
| dc.language.iso | EN | en_US |
| dc.subject.en | Antineoplastic Agents | |
| dc.subject.en | Glioblastoma | |
| dc.subject.en | Humans | |
| dc.subject.en | Leukocyte Elastase | |
| dc.subject.en | Neutrophils | |
| dc.subject.en | Prodrugs | |
| dc.title.en | Neutrophil Elastase-Activatable Prodrugs Based on an Alkoxyamine Platform to Deliver Alkyl Radicals Cytotoxic to Tumor Cells. | |
| dc.title.alternative | J Med Chem | en_US |
| dc.type | Article de revue | en_US |
| dc.subject.hal | Sciences du Vivant [q-bio]/Médecine humaine et pathologie | en_US |
| dc.identifier.pubmed | 35764297 | en_US |
| bordeaux.journal | Journal of Medicinal Chemistry | en_US |
| bordeaux.page | 9253-9266 | en_US |
| bordeaux.volume | 65 | en_US |
| bordeaux.hal.laboratories | Centre de Résonance Magnétique des Systèmes Biologiques (CRMSB) - UMR 5536 | en_US |
| bordeaux.issue | 13 | en_US |
| bordeaux.institution | Université de Bordeaux | en_US |
| bordeaux.institution | CNRS | en_US |
| bordeaux.peerReviewed | oui | en_US |
| bordeaux.inpress | non | en_US |
| bordeaux.import.source | pubmed | |
| hal.identifier | hal-03879852 | |
| hal.version | 1 | |
| hal.date.transferred | 2022-11-30T15:56:32Z | |
| hal.export | true | |
| workflow.import.source | pubmed | |
| dc.rights.cc | Pas de Licence CC | en_US |
| bordeaux.COinS | ctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=Journal%20of%20Medicinal%20Chemistry&rft.date=2022-07-14&rft.volume=65&rft.issue=13&rft.spage=9253-9266&rft.epage=9253-9266&rft.eissn=1520-4804&rft.issn=1520-4804&rft.au=SEREN,%20Seda&JOLY,%20Jean-Patrick&VOISIN,%20Pierre&BOUCHAUD,%20V%C3%A9ronique&AUDRAN,%20G%C3%A9rard&rft.genre=article |
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