Selective p300 inhibitor C646 inhibited HPV E6-E7 genes, altered glucose metabolism and induced apoptosis in cervical cancer cells

Eur J Pharmacol. 2017 Oct 5:812:206-215. doi: 10.1016/j.ejphar.2017.06.005. Epub 2017 Jun 12.

Abstract

High risk HPV infection is a causative factor of cervical cancer. The constitutive expression of HPV E6-E7 genes is important for the maintenance of cancer phenotypes. The cellular transcription co-activator p300 plays a crucial role in the regulation of HPV genes thus it was targeted for the inhibition of HPV-associated cervical cancer. In the present study, HPV positive cervical cells were treated with C646, a selective inhibitor of p300, to investigate its influence on HPV E6-E7 expression and cancer cell growth. Results of RT-qPCR, Western-blot and promoter activity assays showed that C646 inhibited the transcription of HPV E6-E7, which was accompanied with the accumulation of p53 protein. Meanwhile, cell proliferation was suppressed, glucose metabolism was disrupted and apoptosis was induced via the intrinsic pathway. Generally, the anti-cervical cancer potential of C646 was demonstrated and a novel mechanism was proposed in this study.

Keywords: Cervical cancer; Glycolysis; HPV E6-E7; P300 inhibitor; P53 accumulation.

MeSH terms

  • Apoptosis / drug effects*
  • Benzoates / pharmacology*
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • E1A-Associated p300 Protein / antagonists & inhibitors*
  • Enzyme Inhibitors / pharmacology
  • Female
  • Gene Expression Regulation, Neoplastic / drug effects
  • Glucose / metabolism*
  • Glucose Transporter Type 1 / genetics
  • HeLa Cells
  • Humans
  • Membrane Potential, Mitochondrial / drug effects
  • Nitrobenzenes
  • Oncogene Proteins, Viral / genetics*
  • Papillomavirus E7 Proteins / genetics*
  • Pyrazoles / pharmacology*
  • Pyrazolones
  • Repressor Proteins / genetics*
  • Uterine Cervical Neoplasms / pathology*

Substances

  • 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acid
  • Benzoates
  • E6 protein, Human papillomavirus type 16
  • Enzyme Inhibitors
  • Glucose Transporter Type 1
  • Nitrobenzenes
  • Oncogene Proteins, Viral
  • Papillomavirus E7 Proteins
  • Pyrazoles
  • Pyrazolones
  • Repressor Proteins
  • E1A-Associated p300 Protein
  • EP300 protein, human
  • Glucose