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Pregled bibliografske jedinice broj: 966054

Crown ethers reverse P-glycoprotein-mediated multidrug resistance in cancer cells


Guberović, Iva; Marjanović, Marko; Mioč, Marija; Ester, Katja; Martin-Kleiner, Irena; Šumanovac Ramljak, Tatjana; Mlinarić-Majerski, Kata; Kralj, Marijeta
Crown ethers reverse P-glycoprotein-mediated multidrug resistance in cancer cells // Scientific Reports, 8 (2018), 1; 14467, 14 doi:10.1038/s41598-018-32770-y (međunarodna recenzija, članak, znanstveni)


Naslov
Crown ethers reverse P-glycoprotein-mediated multidrug resistance in cancer cells

Autori
Guberović, Iva ; Marjanović, Marko ; Mioč, Marija ; Ester, Katja ; Martin-Kleiner, Irena ; Šumanovac Ramljak, Tatjana ; Mlinarić-Majerski, Kata ; Kralj, Marijeta

Izvornik
Scientific Reports (2045-2322) 8 (2018), 1; 14467, 14

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
Crown-ethers ; P-gp ; MDR

Sažetak
Multidrug resistance (MDR) is a widespread phenomenon exhibited by many cancers and represents a fundamental obstacle for successful cancer treatments. Tumour cells commonly achieve MDR phenotype through overexpression and/or increased activity of ABC transporters. P-glycoprotein transporter (P-gp, ABCB1) is a major cause of MDR and therefore represents a valuable target for MDR reversal. Several naturally occurring potassium ionophores (e.g. salinomycin) were shown to inhibit P-gp effectively. We have previously shown antitumour activity of a number of 18- crown-6 ether compounds that transport potassium ions across membranes. Here we present data on P-gp inhibitory activity of 16 adamantane-substituted monoaza- and diaza-18- crown-6 ether compounds, and their effect on MDR reversal in model cell lines. We show that crown ether activity depends on their lipophilicity as well as on the linker to adamantane moiety. The most active crown ethers were shown to be more effective in sensitising MDR cells to paclitaxel and adriamycin than verapamil, a well-known P-gp inhibitor. Altogether our data demonstrate a novel use of crown ethers for inhibition of P-gp and reversal of MDR phenotype.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biologija, Temeljne medicinske znanosti



POVEZANOST RADA


Projekt / tema
HRZZ-IP-2013-11-5660 - Mulitidisciplinarni pristup otkriću lijekova s ciljanim djelovanjem na matične stanice tumora – uloga transporta kalija (Marijeta Kralj, )

Ustanove
Institut "Ruđer Bošković", Zagreb

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE


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