Quinoides and VEGFR2 TKIs influence the fate of hepatocellular carcinoma and its cancer stem cells

Deniz Cansen Kahraman, Gilles Hanquet, Loïc Jeanmart, Steve Lanners, Peter Šramel, Andrej Boháč, Rengul Cetin-Atalay

Résultats de recherche: Contribution à un journal/une revueArticle

Résumé

Bioactivities of quinoides 1-5 and VEGFR2 TKIs 6-10 in hepatocellular cancer (HCC) and cancer stem cells (HCSCs) were studied. The compounds exhibited IC50 values in μM concentrations in HCC cells. Quinoide 3 was able to eradicate cancer stem cells, similar to the action of the stem cell inhibitor DAPT. However, the more cytotoxic VEFGR TKIs (IC50: 0.4-3.0 μM) including sorafenib, which is the only FDA approved drug for the treatment of HCC, enriched the hepatocellular cancer stem cell population by 2-3 fold after treatment. An aggressiveness factor (AF) was proposed to quantify the characteristics of drug candidates for their ability to eradicate the CSC subpopulation. Considering the tumour heterogeneity and marker positive cancer stem cell like subpopulation enrichment upon treatments in patients, this study emphasises the importance of the chemotherapeutic agent choice acting differentially on all the subpopulations including marker-positive CSCs.

langueAnglais
Pages81-87
Nombre de pages7
journalMedChemComm
Volume8
Numéro1
Date de mise en ligne précoce7 oct. 2016
Les DOIs
étatPublié - 2017

Empreinte digitale

Neoplastic Stem Cells
Liver Neoplasms
Stem cells
Hepatocellular Carcinoma
Inhibitory Concentration 50
Tumor Biomarkers
Pharmaceutical Preparations
Bioactivity
Stem Cells
Therapeutics
Population

Citer ceci

Kahraman, Deniz Cansen ; Hanquet, Gilles ; Jeanmart, Loïc ; Lanners, Steve ; Šramel, Peter ; Boháč, Andrej ; Cetin-Atalay, Rengul. / Quinoides and VEGFR2 TKIs influence the fate of hepatocellular carcinoma and its cancer stem cells. Dans: MedChemComm. 2017 ; Vol 8, Numéro 1. p. 81-87.
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Quinoides and VEGFR2 TKIs influence the fate of hepatocellular carcinoma and its cancer stem cells. / Kahraman, Deniz Cansen; Hanquet, Gilles; Jeanmart, Loïc; Lanners, Steve; Šramel, Peter; Boháč, Andrej; Cetin-Atalay, Rengul.

Dans: MedChemComm, Vol 8, Numéro 1, 2017, p. 81-87.

Résultats de recherche: Contribution à un journal/une revueArticle

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