Mcl-1 is an important determinant of the apoptotic response to the BH3-mimetic molecule HA14-1 in cisplatin-resistant ovarian carcinoma cells

Mol Cancer Ther. 2009 Nov;8(11):3162-70. doi: 10.1158/1535-7163.MCT-09-0493. Epub 2009 Nov 3.

Abstract

Chemoresistance of ovarian carcinoma has been associated previously to the absence of Bcl-x(L) expression downregulation in response to cisplatin. Among BH3-mimetic molecules constituting promising anticancer agents able to inhibit the activity of antiapoptotic Bcl-2 family proteins, we evaluated the effect of one of them, HA14-1, on various ovarian carcinoma cell lines. In response to HA14-1, the cisplatin-resistant IGROV1-R10 cell line underwent massive cell death, whereas other cell lines presented a partial response (IGROV1, SKOV3, and A2780) or did not respond to this molecule (OAW42 and OAW42-R). However, the expression of HA14-1 targets (Bcl-2 and Bcl-x(L)) did not correlate to these different responses. In contrast, cell death was associated with the disappearance of Mcl-1 after exposure to HA14-1. We showed that, in the HA14-1 nonresponsive cell lines (SKOV3 and OAW42), small interfering RNA-mediated Mcl-1 downregulation allowed HA14-1-induced massive apoptosis in the absence of chemotherapy. Furthermore, cisplatin-induced Mcl-1 downregulation was also able to sensitize highly chemoresistant SKOV3 cells to HA14-1. Taken together, these results show that Bcl-x(L) and Mcl-1 are able to cooperate to protect ovarian carcinoma cells against oncogenic stress or chemotherapy-induced apoptosis and suggest that the development of multitargeted strategies directed against these two antiapoptotic proteins may constitute a major challenge for the therapeutic care of chemoresistant ovarian carcinomas. BH3-mimetic compounds represent promising tools for this purpose either on their own (direct or indirect pan-inhibitors) or in combination with new drugs aiming to inactivate Mcl-1.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenocarcinoma / drug therapy
  • Adenocarcinoma / genetics
  • Adenocarcinoma / metabolism
  • Adenocarcinoma / pathology
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology
  • Apoptosis / drug effects*
  • Apoptosis / physiology
  • Autophagy / drug effects
  • Autophagy / physiology
  • Benzopyrans / administration & dosage
  • Benzopyrans / pharmacology*
  • Cell Death / drug effects
  • Cell Death / physiology
  • Cell Line, Tumor
  • Cisplatin / administration & dosage
  • Cisplatin / pharmacology*
  • Down-Regulation
  • Drug Resistance, Neoplasm
  • Drug Synergism
  • Female
  • Flow Cytometry
  • Humans
  • Myeloid Cell Leukemia Sequence 1 Protein
  • Nitriles / administration & dosage
  • Nitriles / pharmacology*
  • Ovarian Neoplasms / drug therapy*
  • Ovarian Neoplasms / genetics
  • Ovarian Neoplasms / metabolism
  • Ovarian Neoplasms / pathology
  • Proto-Oncogene Proteins c-bcl-2 / biosynthesis*
  • Proto-Oncogene Proteins c-bcl-2 / genetics
  • RNA Interference
  • RNA, Small Interfering / administration & dosage
  • RNA, Small Interfering / genetics
  • Transfection
  • bcl-X Protein / biosynthesis

Substances

  • Benzopyrans
  • Myeloid Cell Leukemia Sequence 1 Protein
  • Nitriles
  • Proto-Oncogene Proteins c-bcl-2
  • RNA, Small Interfering
  • bcl-X Protein
  • ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate
  • Cisplatin