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Pregled bibliografske jedinice broj: 972442

Crown ether compound 613 as a small molecule with good antitumor potential: investigation of membrane perturbation and changes in ion homeostasis


Katja Ester, Marija Mioč, Jelena Gabrilo, Lidija Uzelac, Marko Marjanović, Pavel Spurny, Daniel Bonhenry, Tatjana Šumanovac-Ramljak, Jost Ludwig, Kata Mlinarić-Majerski and Marijeta Kralj
Crown ether compound 613 as a small molecule with good antitumor potential: investigation of membrane perturbation and changes in ion homeostasis // COST BM 1406 Eight Meeting Abstract Book
Seillac, Francuska, 2018. str. 24-24 (predavanje, međunarodna recenzija, sažetak, ostalo)


CROSBI ID: 972442 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
Crown ether compound 613 as a small molecule with good antitumor potential: investigation of membrane perturbation and changes in ion homeostasis

Autori
Katja Ester, Marija Mioč, Jelena Gabrilo, Lidija Uzelac, Marko Marjanović, Pavel Spurny, Daniel Bonhenry, Tatjana Šumanovac-Ramljak, Jost Ludwig, Kata Mlinarić-Majerski and Marijeta Kralj

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, ostalo

Izvornik
COST BM 1406 Eight Meeting Abstract Book / - , 2018, 24-24

Skup
COST BM 1406 8th Meeting

Mjesto i datum
Seillac, Francuska, 9-11.10.2018

Vrsta sudjelovanja
Predavanje

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
crown ether, breast cancer, membrane potential, cell death, ionophore

Sažetak
Crown ethers represent small molecules that hold promising antitumor potential. Among other modes of action, crown ethers can act as ionophores, i.e. disturbing ion homeostasis and disrupting biological membranes. We showed that crown ethers inhibit P-glycoprotein and reverse the multidrug resistance in cancer cells. Based on the previous in vitro screening, we identified the proprietary crown ether compound 613 as a potential antitumor drug. Inhibition of tumor growth was confirmed on the panel of breast tumor cells, and in an in vivo mouse model. To unravel the mechanism of action, we choose an approach based on its structure: we postulated that 613 could 1) potentially bind and move ions through the membrane and change the ion homeostasis, and 2) cause perturbations of the lipid membranes throughout the cell due to its hydrophobicity. We found that compound 613 induced K+ and Na+ fluxes and modulated resting potential of cells. Physical disturbance of lipid membranes throughout the cell was demonstrated by increase in plasma membrane permeability and impairment of mitochondrial functions. The importance and/or interplay of the two mechanisms responsible for cytotoxicity yet awaits to be resolved.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biologija, Biotehnologija u biomedicini (prirodno područje, biomedicina i zdravstvo, biotehničko područje)



POVEZANOST RADA


Projekti:
HRZZ-IP-2013-11-5660 - Mulitidisciplinarni pristup otkriću lijekova s ciljanim djelovanjem na matične stanice tumora – uloga transporta kalija (MultiCaST) (Kralj, Marijeta, HRZZ - 2013-11) ( POIROT)

Ustanove:
Institut "Ruđer Bošković", Zagreb


Citiraj ovu publikaciju

Katja Ester, Marija Mioč, Jelena Gabrilo, Lidija Uzelac, Marko Marjanović, Pavel Spurny, Daniel Bonhenry, Tatjana Šumanovac-Ramljak, Jost Ludwig, Kata Mlinarić-Majerski and Marijeta Kralj
Crown ether compound 613 as a small molecule with good antitumor potential: investigation of membrane perturbation and changes in ion homeostasis // COST BM 1406 Eight Meeting Abstract Book
Seillac, Francuska, 2018. str. 24-24 (predavanje, međunarodna recenzija, sažetak, ostalo)
Katja Ester, Marija Mioč, Jelena Gabrilo, Lidija Uzelac, Marko Marjanović, Pavel Spurny, Daniel Bonhenry, Tatjana Šumanovac-Ramljak, Jost Ludwig, Kata Mlinarić-Majerski and Marijeta Kralj (2018) Crown ether compound 613 as a small molecule with good antitumor potential: investigation of membrane perturbation and changes in ion homeostasis. U: COST BM 1406 Eight Meeting Abstract Book.
@article{article, year = {2018}, pages = {24-24}, keywords = {crown ether, breast cancer, membrane potential, cell death, ionophore}, title = {Crown ether compound 613 as a small molecule with good antitumor potential: investigation of membrane perturbation and changes in ion homeostasis}, keyword = {crown ether, breast cancer, membrane potential, cell death, ionophore}, publisherplace = {Seillac, Francuska} }
@article{article, year = {2018}, pages = {24-24}, keywords = {crown ether, breast cancer, membrane potential, cell death, ionophore}, title = {Crown ether compound 613 as a small molecule with good antitumor potential: investigation of membrane perturbation and changes in ion homeostasis}, keyword = {crown ether, breast cancer, membrane potential, cell death, ionophore}, publisherplace = {Seillac, Francuska} }




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