Is antitumor Pt(IV) complex containing two axial lonidamine ligands a true dual- or multi-action prodrug?

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68081707%3A_____%2F22%3A00559611" target="_blank" >RIV/68081707:_____/22:00559611 - isvavai.cz</a>

Výsledek na webu

<a href="https://academic.oup.com/metallomics/article/14/7/mfac048/6618656?login=true" target="_blank" >https://academic.oup.com/metallomics/article/14/7/mfac048/6618656?login=true</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1093/mtomcs/mfac048" target="_blank" >10.1093/mtomcs/mfac048</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Is antitumor Pt(IV) complex containing two axial lonidamine ligands a true dual- or multi-action prodrug?

Popis výsledku v původním jazyce

This work studied the mechanism of action of a Pt(IV) complex 2 bearing two axial lonidamine ligands, which are selective inhibitors of aerobic glycolysis. The presence of two lonidamine ligands in 2 compared to the parent Pt(II) complex increased its antiproliferative activity, cellular accumulation, and changed its cell cycle profile and mechanism of cell death. In 3D cell culture, 2 showed exceptional antiproliferative activity with IC50 values as low as 1.6 mu M in MCF7 cells. The study on the influence of the lonidamine ligands in the Pt complex on glycolysis showed only low potency of ligands to affect metabolic processes in cancer cells, making the investigated complex, not a dual- or multi-action prodrug. However, the Pt(IV) prodrug effectively delivers the cytotoxic Pt(II) complex into cancer cells.

Název v anglickém jazyce

Is antitumor Pt(IV) complex containing two axial lonidamine ligands a true dual- or multi-action prodrug?

Popis výsledku anglicky

This work studied the mechanism of action of a Pt(IV) complex 2 bearing two axial lonidamine ligands, which are selective inhibitors of aerobic glycolysis. The presence of two lonidamine ligands in 2 compared to the parent Pt(II) complex increased its antiproliferative activity, cellular accumulation, and changed its cell cycle profile and mechanism of cell death. In 3D cell culture, 2 showed exceptional antiproliferative activity with IC50 values as low as 1.6 mu M in MCF7 cells. The study on the influence of the lonidamine ligands in the Pt complex on glycolysis showed only low potency of ligands to affect metabolic processes in cancer cells, making the investigated complex, not a dual- or multi-action prodrug. However, the Pt(IV) prodrug effectively delivers the cytotoxic Pt(II) complex into cancer cells.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

10608 - Biochemistry and molecular biology

Projekt

<a href="/cs/project/GC20-14082J" target="_blank" >GC20-14082J: Vývoj nových, cílených vícejaderných komplexů platiny a ruthenia pro chemoterapii rakoviny. Mechanimus působení</a><br>

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2022

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Metallomics

ISSN

1756-5901

e-ISSN

1756-591X

Svazek periodika

14

Číslo periodika v rámci svazku

7

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

12

Strana od-do

mfac048

Kód UT WoS článku

000827780700001

EID výsledku v databázi Scopus

2-s2.0-85134721431