Literature DB >> 24692700

Synergistic inhibition of HCC and liver cancer stem cell proliferation by targeting RAS/RAF/MAPK and WNT/β-catenin pathways.

Roberto Galuppo1, Erin Maynard, Malay Shah, Michael F Daily, Changguo Chen, Brett T Spear, Roberto Gedaly.   

Abstract

BACKGROUND/AIM: The aim of this study is to find synergistic effect using FH535 and sorafenib by targeting the RAS/RAF/MAPK and WNT/β-catenin pathways.
MATERIALS AND METHODS: 3H-Thymidine incorporation assays were performed to address Huh7 and liver cancer stem cell (LCSC) inhibition using FH535 and sorafenib, alone and in combination. Calcusyn analysis was used to calculate the combination index (CI). A western blot assay was performed to check for potential targets.
RESULTS: FH535 and sorafenib caused inhibition of Huh7 and LCSC. Combination therapy was significantly better than monotherapy in inhibition of HuH7. Combination with sorafenib and FH535 was found to be synergistic in inhibition of LCSC with a CI of less than 1. The western blot assay demonstrated enhanced cleaved poly (ADP-ribose) polymerase (PARP) and inhibition of cyclin D1, B-cell lymphoma 2 (Bcl2), survivin and cellular myelocytomatosis oncogene (c-MYC).
CONCLUSION: FH535 and sorafenib combination produced synergistic effect on inhibition of HCC and LCSC. Our study demonstrated that FH535 can induce apoptosis in these two different hepatocellular carcinoma (HCC) cell lines.

Entities:  

Keywords:  Hepatocellular carcinoma; PI-103; PKI-587; RAS/RAF/MAPK; epidermal growth factor; liver cancer stem cells; mTOR complex 1; mTOR complex 2; rapamycin; sorafenib

Mesh:

Substances:

Year:  2014        PMID: 24692700      PMCID: PMC5733784     

Source DB:  PubMed          Journal:  Anticancer Res        ISSN: 0250-7005            Impact factor:   2.480


  21 in total

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Authors:  Fumi Takahashi-Yanaga; Michael Kahn
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2.  PI-103 and sorafenib inhibit hepatocellular carcinoma cell proliferation by blocking Ras/Raf/MAPK and PI3K/AKT/mTOR pathways.

Authors:  Roberto Gedaly; Paul Angulo; Jonathan Hundley; Michael F Daily; Changguo Chen; Alvaro Koch; B Mark Evers
Journal:  Anticancer Res       Date:  2010-12       Impact factor: 2.480

3.  Ras pathway activation in hepatocellular carcinoma and anti-tumoral effect of combined sorafenib and rapamycin in vivo.

Authors:  Pippa Newell; Sara Toffanin; Augusto Villanueva; Derek Y Chiang; Beatriz Minguez; Laia Cabellos; Radoslav Savic; Yujin Hoshida; Kiat Hon Lim; Pedro Melgar-Lesmes; Steven Yea; Judit Peix; Kemal Deniz; M Isabel Fiel; Swan Thung; Clara Alsinet; Victoria Tovar; Vincenzo Mazzaferro; Jordi Bruix; Sasan Roayaie; Myron Schwartz; Scott L Friedman; Josep M Llovet
Journal:  J Hepatol       Date:  2009-06-12       Impact factor: 25.083

Review 4.  Targeting cancer stem cells by inhibiting Wnt, Notch, and Hedgehog pathways.

Authors:  Naoko Takebe; Pamela J Harris; Ronald Q Warren; S Percy Ivy
Journal:  Nat Rev Clin Oncol       Date:  2010-12-14       Impact factor: 66.675

5.  A small-molecule inhibitor of Tcf/beta-catenin signaling down-regulates PPARgamma and PPARdelta activities.

Authors:  Shlomo Handeli; Julian A Simon
Journal:  Mol Cancer Ther       Date:  2008-03       Impact factor: 6.261

Review 6.  Hepatocellular carcinoma.

Authors:  Josep M Llovet; Andrew Burroughs; Jordi Bruix
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7.  A cell initiating human acute myeloid leukaemia after transplantation into SCID mice.

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Journal:  Nature       Date:  1994-02-17       Impact factor: 49.962

Review 8.  Role of the microenvironment in the pathogenesis and treatment of hepatocellular carcinoma.

Authors:  Virginia Hernandez-Gea; Sara Toffanin; Scott L Friedman; Josep M Llovet
Journal:  Gastroenterology       Date:  2013-01-09       Impact factor: 22.682

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Authors:  Rachel H Giles; Johan H van Es; Hans Clevers
Journal:  Biochim Biophys Acta       Date:  2003-06-05

10.  Sorafenib in advanced hepatocellular carcinoma.

Authors:  Josep M Llovet; Sergio Ricci; Vincenzo Mazzaferro; Philip Hilgard; Edward Gane; Jean-Frédéric Blanc; Andre Cosme de Oliveira; Armando Santoro; Jean-Luc Raoul; Alejandro Forner; Myron Schwartz; Camillo Porta; Stefan Zeuzem; Luigi Bolondi; Tim F Greten; Peter R Galle; Jean-François Seitz; Ivan Borbath; Dieter Häussinger; Tom Giannaris; Minghua Shan; Marius Moscovici; Dimitris Voliotis; Jordi Bruix
Journal:  N Engl J Med       Date:  2008-07-24       Impact factor: 91.245

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  25 in total

Review 1.  Roles of mitochondria in liver cancer stem cells.

Authors:  Ching-Wen Chang; Jeng-Fan Lo; Xin Wei Wang
Journal:  Differentiation       Date:  2019-05-30       Impact factor: 3.880

2.  IQGAP1 gene silencing induces apoptosis and decreases the invasive capacity of human hepatocellular carcinoma cells.

Authors:  Khairy Ma Zoheir; Ahmed A Abd-Rabou; Gamaleldin I Harisa; Ashok Kumar; Sheikh Fayaz Ahmad; Mushtaq Ahmad Ansari; Adel R Abd-Allah
Journal:  Tumour Biol       Date:  2016-08-03

3.  BEZ235 increases sorafenib inhibition of hepatocellular carcinoma cells by suppressing the PI3K/AKT/mTOR pathway.

Authors:  Amin Li; Rongbo Zhang; Yinci Zhang; Xueke Liu; Ruikai Wang; Jiachang Liu; Xinkuang Liu; Yinghai Xie; Weiya Cao; Ruyue Xu; Yongfang Ma; Wenpeng Cai; Binquan Wu; Shuyu Cai; Xiaolong Tang
Journal:  Am J Transl Res       Date:  2019-09-15       Impact factor: 4.060

4.  Carboxypeptidase A4 promotes proliferation and stem cell characteristics of hepatocellular carcinoma.

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Journal:  Int J Exp Pathol       Date:  2019-05-06       Impact factor: 1.925

5.  N-Aryl benzenesulfonamide inhibitors of [3H]-thymidine incorporation and β-catenin signaling in human hepatocyte-derived Huh-7 carcinoma cells.

Authors:  Liliia M Kril; Valery Vilchez; Jieyun Jiang; Lilia Turcios; Changguo Chen; Vitaliy M Sviripa; Wen Zhang; Chunming Liu; Brett Spear; David S Watt; Roberto Gedaly
Journal:  Bioorg Med Chem Lett       Date:  2015-07-26       Impact factor: 2.823

Review 6.  Mechanisms of hepatocellular carcinoma and challenges and opportunities for molecular targeted therapy.

Authors:  Chuan Chen; Ge Wang
Journal:  World J Hepatol       Date:  2015-07-28

Review 7.  Targeting Wnt/β-catenin pathway in hepatocellular carcinoma treatment.

Authors:  Valery Vilchez; Lilia Turcios; Francesc Marti; Roberto Gedaly
Journal:  World J Gastroenterol       Date:  2016-01-14       Impact factor: 5.742

8.  Downregulation of TMEM220 promotes tumor progression in Hepatocellular Carcinoma.

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Journal:  Cancer Gene Ther       Date:  2021-07-28       Impact factor: 5.854

Review 9.  Apoptotic death of cancer stem cells for cancer therapy.

Authors:  Ying-Chun He; Fang-Liang Zhou; Yi Shen; Duan-Fang Liao; Deliang Cao
Journal:  Int J Mol Sci       Date:  2014-05-12       Impact factor: 5.923

Review 10.  Reversible Human TGF-β Signal Shifting between Tumor Suppression and Fibro-Carcinogenesis: Implications of Smad Phospho-Isoforms for Hepatic Epithelial-Mesenchymal Transitions.

Authors:  Katsunori Yoshida; Miki Murata; Takashi Yamaguchi; Koichi Matsuzaki; Kazuichi Okazaki
Journal:  J Clin Med       Date:  2016-01-12       Impact factor: 4.241

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