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Cytotoxic effect of a family of peroxisome proliferator-activated receptor antagonists in colorectal and pancreatic cancer cell lines.

Alessandra AmmazzalorsoLaura De LellisRosalba FlorioIsabella BrunoBarbara De FilippisMarialuigia FantacuzziLetizia GiampietroCristina MaccalliniSilvia PercontiFabio VerginelliAlessandro CamaRosa Amoroso
Published in: Chemical biology & drug design (2017)
Recent studies report an interesting role of peroxisome proliferator-activated receptor (PPAR) antagonists in different tumor models, being these compounds able to perturb metabolism and viability in cancer cells. In this work, the identification of a novel PPAR antagonist, showing inhibitory activity on PPARα and a weaker antagonism on PPARγ, is described. The activity of this compound and of a series of chemical analogues was investigated in selected tumor cell lines, expressing both PPARα and PPARγ. Data obtained show a dose-dependent cytotoxic effect of the novel PPAR antagonist in colorectal and pancreatic cancer models.
Keyphrases
  • insulin resistance
  • fatty acid
  • metabolic syndrome
  • mass spectrometry
  • machine learning
  • big data
  • high resolution
  • binding protein