All-trans retinoic acid and protein kinase C α/β1 inhibitor combined treatment targets cancer stem cells and impairs breast tumor progression

Sci Rep. 2021 Mar 15;11(1):6044. doi: 10.1038/s41598-021-85344-w.

Abstract

Breast cancer is the leading cause of cancer death among women worldwide. Blocking a single signaling pathway is often an ineffective therapy, especially in the case of aggressive or drug-resistant tumors. Since we have previously described the mechanism involved in the crosstalk between Retinoic Acid system and protein kinase C (PKC) pathway, the rationale of our study was to evaluate the effect of combining all-trans-retinoic acid (ATRA) with a classical PCK inhibitor (Gö6976) in preclinical settings. Employing hormone-independent mammary cancer models, Gö6976 and ATRA combined treatment induced a synergistic reduction in proliferative potential that correlated with an increased apoptosis and RARs modulation towards an anti-oncogenic profile. Combined treatment also impairs growth, self-renewal and clonogenicity potential of cancer stem cells and reduced tumor growth, metastatic spread and cancer stem cells frequency in vivo. An in-silico analysis of "Kaplan-Meier plotter" database indicated that low PKCα together with high RARα mRNA expression is a favorable prognosis factor for hormone-independent breast cancer patients. Here we demonstrate that a classical PKC inhibitor potentiates ATRA antitumor effects also targeting cancer stem cells growth, self-renewal and frequency.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology*
  • Cell Line, Tumor
  • Female
  • Mammary Neoplasms, Experimental* / drug therapy
  • Mammary Neoplasms, Experimental* / enzymology
  • Mice
  • Mice, Inbred BALB C
  • Neoplasm Proteins* / antagonists & inhibitors
  • Neoplasm Proteins* / metabolism
  • Neoplastic Stem Cells / enzymology*
  • Protein Kinase C beta* / antagonists & inhibitors
  • Protein Kinase C beta* / metabolism
  • Protein Kinase C-alpha* / antagonists & inhibitors
  • Protein Kinase C-alpha* / metabolism
  • Protein Kinase Inhibitors / pharmacology
  • Tretinoin / pharmacology

Substances

  • Neoplasm Proteins
  • Protein Kinase Inhibitors
  • Tretinoin
  • Prkca protein, mouse
  • Prkcb protein, mouse
  • Protein Kinase C beta
  • Protein Kinase C-alpha