Literature DB >> 29976629

The Dual PI3K/mToR Inhibitor Omipalisib/GSK2126458 Inhibits Clonogenic Growth in Oncogenically-transformed Cells from Neurocutaneous Melanocytosis.

Dipanjan Basu1, Cláudia M Salgado2, Bruce Bauer3, Yasmin Khakoo4,5, Janki R Patel6, Ryan M Hoehl6, Dominique M Bertolini6, Joie Zabec6, Morgan R Brzozowski6, Miguel Reyes-Múgica2.   

Abstract

BACKGROUND: Omipalisib has been found to affect the viability of cancer cells. However, its effect on clonogenicity - a feature of cancer stem cells, is not clear. Cells isolated from neurocutaneous melanocytosis (NCM) patients' lesions grow clonogenically. The aim of this study was to investigate the effect of omipalisib treatment on clonogenic growth of NCM cells in vitro.
MATERIALS AND METHODS: Clonogenic growth efficiency was evaluated by colony formation assays with or without specific growth factors. Activation of MEK and Akt was determined by immunoblots. Colony formation and cell viability were assessed upon pharmacological inhibition of MEK, Akt and mToR.
RESULTS: Clonogenicity appeared to depend on bFGF and IGF1signaling through ERK and Akt. Omipalisib treatment prevented colony formation and induced autophagic cell death.
CONCLUSION: Signaling through Akt is important for survival of clonogenic cells in NCM, and omipalisib treatment as a monotherapy or in combination with MEK162 could be an effective therapeutic strategy to inhibit clonogenic growth. Copyright
© 2018, International Institute of Anticancer Research (Dr. George J. Delinasios), All rights reserved.

Entities:  

Keywords:  Clonogenicity; MEK162; neurocutaneous melanocytosis; omipalisib

Mesh:

Substances:

Year:  2018        PMID: 29976629      PMCID: PMC6070711          DOI: 10.21873/cgp.20082

Source DB:  PubMed          Journal:  Cancer Genomics Proteomics        ISSN: 1109-6535            Impact factor:   4.069


  24 in total

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7.  Omipalisib Inhibits Esophageal Squamous Cell Carcinoma Growth Through Inactivation of Phosphoinositide 3-Kinase (PI3K)/AKT/Mammalian Target of Rapamycin (mTOR) and ERK Signaling.

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