Flavopiridol reduces malignant transformation of the esophageal mucosa in p27 knockout mice

Oncogene. 2005 Mar 3;24(10):1683-8. doi: 10.1038/sj.onc.1208375.

Abstract

The cyclin-dependent kinase (cdk) inhibitor p27 preferentially inactivates cdk complexes required for progression through the G1/S transition. Loss of p27 is associated with aggressive behavior in a variety of tumors, including Barrett's associated adenocarcinoma (BAA). We have previously shown that gastroduodenal-esophageal reflux (GDER) together with N-methyl-N-benzylnitrosamine (MBN) induces Barrett's esophagus (BE) and malignant transformation of the esophageal mucosa in mice. This process is enhanced in a p27 null background. Here, we show that chronic flavopiridol administration sharply reduced the prevalence of BE in GDER/MBN-treated p27 knockout mice when compared to animals treated with diluent only (7 vs 26%, P=0.0079). Similarly, flavopiridol reduced the prevalence of BAA (11 vs 32%, P=0.0098) and overall cancer prevalence (15 vs 60%, P<0.0001). In addition, appropriate molecular targeting by flavopiridol in tumor cells was confirmed by downregulation of cyclin D1, a known target of this pan-cdk inhibitor. The results of this study represent the experimental basis for chemoprevention with cdk inhibitors in human BE and BAA.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adenocarcinoma / prevention & control
  • Animals
  • Anticarcinogenic Agents / pharmacology*
  • Barrett Esophagus / prevention & control
  • Carcinoma, Squamous Cell / prevention & control
  • Cell Cycle Proteins / physiology*
  • Cell Transformation, Neoplastic*
  • Cyclin D1 / physiology
  • Cyclin-Dependent Kinase Inhibitor p27
  • Esophageal Neoplasms / prevention & control*
  • Flavonoids / pharmacology*
  • Mice
  • Phosphorylation
  • Piperidines / pharmacology*
  • Retinoblastoma Protein / metabolism
  • Tumor Suppressor Proteins / physiology*

Substances

  • Anticarcinogenic Agents
  • Cdkn1b protein, mouse
  • Cell Cycle Proteins
  • Flavonoids
  • Piperidines
  • Retinoblastoma Protein
  • Tumor Suppressor Proteins
  • Cyclin D1
  • Cyclin-Dependent Kinase Inhibitor p27
  • alvocidib