Astemizole-based anticancer therapy for hepatocellular carcinoma (HCC), and Eag1 channels as potential early-stage markers of HCC

Tumour Biology : the Journal of the International Society for Oncodevelopmental Biology and Medicine
María de Guadalupe Chávez-LópezJavier Camacho

Abstract

Hepatocellular carcinoma (HCC) has very poor prognosis. Astemizole has gained great interest as a potential anticancer drug because it targets several proteins involved in cancer including the Eag1 (ether à-go-go-1) potassium channel that is overexpressed in human HCC. Eag1 channels are regulated by cancer etiological factors and have been proposed as early tumor markers. Here, we found that HepG2 and HuH-7 HCC cells displayed Eag1 messenger RNA (mRNA) and protein expression, determined by real-time RT-PCR and immunochemistry, respectively. Astemizole inhibited human HCC cell proliferation (assessed by metabolic activity assay) and induced apoptosis (studied with flow cytometry) in both cell lines. The subcellular Eag1 protein localization was modified by astemizole in the HepG2 cells. The treatment with astemizole prevented diethylnitrosamine (DEN)-induced rat HCC development in vivo (followed by studying γ-glutamyl transpeptidase (GGT) activity). The Eag1 mRNA and protein levels were increased in most DEN-treated groups but decreased after astemizole treatment. GGT activity was decreased by astemizole. The Eag1 protein was detected in cirrhotic and dysplastic rat livers. Astemizole might have clinical utility for HCC preventi...Continue Reading

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Citations

Feb 18, 2016·Oxidative Medicine and Cellular Longevity·Ana RamírezJavier Camacho
Jun 29, 2016·European Biophysics Journal : EBJ·Franziska Hartung, Luis A Pardo
Jul 23, 2016·European Biophysics Journal : EBJ·Joanna NappFrauke Alves
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Feb 25, 2017·Tumour Biology : the Journal of the International Society for Oncodevelopmental Biology and Medicine·Gabriela Velasco-LoydenVictoria Chagoya de Sánchez
Jun 8, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Qing-Ye ZhangHong-Yu Zhang
Jan 25, 2020·Genes·María de Guadalupe Chávez-LópezJavier Camacho
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Jun 13, 2020·Frontiers in Pharmacology·Franziska HartungLuis A Pardo
Jun 21, 2018·Blood Cancer Journal·Isabelle LaverdièreKolja Eppert
Jan 1, 2021·Frontiers in Cell and Developmental Biology·Magdalena BachmannErich Gulbins
Sep 28, 2018·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Junli XuShuixiang He

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