Bcl-xL deamidation is a critical switch in the regulation of the response to DNA damage

Cell. 2002 Oct 4;111(1):51-62. doi: 10.1016/s0092-8674(02)00972-8.

Abstract

The therapeutic value of DNA-damaging antineoplastic agents is dependent upon their ability to induce tumor cell apoptosis while sparing most normal tissues. Here, we show that a component of the apoptotic response to these agents in several different types of tumor cells is the deamidation of two asparagines in the unstructured loop of Bcl-xL, and we demonstrate that deamidation of these asparagines imports susceptibility to apoptosis by disrupting the ability of Bcl-xL to block the proapoptotic activity of BH3 domain-only proteins. Conversely, Bcl-xL deamidation is actively suppressed in fibroblasts, and suppression of deamidation is an essential component of their resistance to DNA damage-induced apoptosis. Our results suggest that the regulation of Bcl-xL deamidation has a critical role in the tumor-specific activity of DNA-damaging antineoplastic agents.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Antineoplastic Agents / pharmacology
  • Apoptosis
  • Asparagine / chemistry
  • Asparagine / metabolism
  • Cisplatin / pharmacology
  • DNA Damage*
  • Dose-Response Relationship, Drug
  • Fibroblasts / metabolism
  • Gene Expression Regulation*
  • Humans
  • Immunoblotting
  • Microscopy, Fluorescence
  • Molecular Sequence Data
  • Oligonucleotides, Antisense / pharmacology
  • Peptides / chemistry
  • Plasmids / metabolism
  • Protein Structure, Tertiary
  • Proto-Oncogene Proteins c-bcl-2 / metabolism*
  • Sequence Homology, Amino Acid
  • Time Factors
  • Transfection
  • Tumor Cells, Cultured
  • bcl-X Protein

Substances

  • Antineoplastic Agents
  • BCL2L1 protein, human
  • Oligonucleotides, Antisense
  • Peptides
  • Proto-Oncogene Proteins c-bcl-2
  • bcl-X Protein
  • Asparagine
  • Cisplatin