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N-Heterocyclic Carbene-Polyethylenimine Platinum Complexes with Potent in Vitro and in Vivo Antitumor Efficacy

dc.contributor.authorCHEKKAT, N.
dc.contributor.authorDAHM, G.
dc.contributor.authorCHARDON, E.
dc.contributor.authorWANTZ, M.
dc.contributor.authorSITZ, J.
dc.contributor.authorDECOSSAS, M.
dc.contributor.authorLAMBERT, O.
dc.contributor.authorFRISCH, B.
dc.contributor.authorRUBBIANI, R.
dc.contributor.authorGASSER, G.
dc.contributor.authorGUICHARD, Gilles
dc.contributor.authorFOURNEL, S.
dc.contributor.authorBELLEMIN-LAPONNAZ, S.
dc.date.accessioned2020-09-03T07:56:23Z
dc.date.available2020-09-03T07:56:23Z
dc.date.issued2016
dc.identifier.issn1043-1802
dc.identifier.urihttps://oskar-bordeaux.fr/handle/20.500.12278/10890
dc.description.abstractEnThe current interest for platinum N-heterocyclic carbene complexes in cancer research stems from their impressive toxicity reported against a range of different human cancer cells. To date, the demonstration of their in vivo efficacy relative to that of established platinum-based drugs has not been specifically addressed. Here, we introduce an innovative approach to increase the NHC-Pt complex potency whereby multiple NHC-Pt(II) complexes are coordinated along a polyethylenimine polymer (PEI) chain. We show that such NHC-Pt(II)-PEI conjugates induce human cancer cell death in vitro and in vivo in a xenograft mouse model with no observable side effects in contrast to oxaliplatin. Additional studies indicate nucleus and mitochondria targeting and suggest various mechanisms of action compared to classical platinum-based anticancer drugs.
dc.language.isoen
dc.title.enN-Heterocyclic Carbene-Polyethylenimine Platinum Complexes with Potent in Vitro and in Vivo Antitumor Efficacy
dc.typeArticle de revue
dc.identifier.doi10.1021/acs.bioconjchem.6b00320
dc.subject.halChimie/Matériaux
bordeaux.journalBioconjugate Chemistry
bordeaux.page1942-1948
bordeaux.volume27
bordeaux.hal.laboratoriesInstitut de Chimie & de Biologie des Membranes & des Nano-objets (CBMN) - UMR 5248*
bordeaux.hal.laboratoriesInstitut de Chimie & de Biologie des Membranes & des Nano-objets (CBMN, UMR 5248)
bordeaux.issue8
bordeaux.institutionUniversité de Bordeaux
bordeaux.institutionBordeaux INP
bordeaux.COinSctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=Bioconjugate%20Chemistry&rft.date=2016&rft.volume=27&rft.issue=8&rft.spage=1942-1948&rft.epage=1942-1948&rft.eissn=1043-1802&rft.issn=1043-1802&rft.au=CHEKKAT,%20N.&DAHM,%20G.&CHARDON,%20E.&WANTZ,%20M.&SITZ,%20J.&rft.genre=article


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