The plant isoflavenoid genistein activates p53 and Chk2 in an ATM-dependent manner

J Biol Chem. 2001 Feb 16;276(7):4828-33. doi: 10.1074/jbc.M004894200. Epub 2000 Nov 28.

Abstract

Genistein is an isoflavenoid that is abundant in soy beans. Genistein has been reported to have a wide range of biological activities and to play a role in the diminished incidence of breast cancer in populations that consume a soy-rich diet. Genistein was originally identified as an inhibitor of tyrosine kinases; however, it also inhibits topoisomerase II by stabilizing the covalent DNA cleavage complex, an event predicted to cause DNA damage. The topoisomerase II inhibitor etoposide acts in a similar manner. Here we show that genistein induces the up-regulation of p53 protein, phosphorylation of p53 at serine 15, activation of the sequence-specific DNA binding properties of p53, and phosphorylation of the hCds1/Chk2 protein kinase at threonine 68. Phosphorylation and activation of p53 and phosphorylation of Chk2 were not observed in ATM-deficient cells. In contrast, the topoisomerase II inhibitor etoposide induced phosphorylation of p53 and Chk2 in ATM-positive and ATM-deficient cells. In addition, genistein-treated ATM-deficient cells were significantly more susceptible to genistein-induced killing than were ATM-positive cells. Together our data suggest that ATM is required for activation of a DNA damage-induced pathway that activates p53 and Chk2 in response to genistein.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Androstadienes / pharmacology
  • Ataxia Telangiectasia Mutated Proteins
  • Benzoquinones
  • Caffeine / pharmacology
  • Cell Cycle Proteins
  • Cell Line
  • Checkpoint Kinase 2
  • DNA Fragmentation
  • DNA-Binding Proteins
  • Enzyme Inhibitors / pharmacology*
  • Etoposide / pharmacology
  • Genistein / pharmacology*
  • Humans
  • Lactams, Macrocyclic
  • Mutation
  • Phosphorylation
  • Plants, Medicinal
  • Protein Kinases / metabolism*
  • Protein Serine-Threonine Kinases / genetics
  • Protein Serine-Threonine Kinases / physiology*
  • Protein-Tyrosine Kinases / antagonists & inhibitors
  • Quinones / pharmacology
  • Rifabutin / analogs & derivatives
  • Topoisomerase II Inhibitors
  • Tumor Suppressor Protein p53 / metabolism*
  • Tumor Suppressor Proteins
  • Wortmannin

Substances

  • Androstadienes
  • Benzoquinones
  • Cell Cycle Proteins
  • DNA-Binding Proteins
  • Enzyme Inhibitors
  • Lactams, Macrocyclic
  • Quinones
  • Topoisomerase II Inhibitors
  • Tumor Suppressor Protein p53
  • Tumor Suppressor Proteins
  • Rifabutin
  • Caffeine
  • Etoposide
  • herbimycin
  • Genistein
  • Protein Kinases
  • Checkpoint Kinase 2
  • Protein-Tyrosine Kinases
  • ATM protein, human
  • Ataxia Telangiectasia Mutated Proteins
  • CHEK2 protein, human
  • Protein Serine-Threonine Kinases
  • Wortmannin