Structure of the Bcr-Abl oncoprotein oligomerization domain

Nat Struct Biol. 2002 Feb;9(2):117-20. doi: 10.1038/nsb747.

Abstract

The Bcr-Abl oncoprotein is responsible for a wide range of human leukemias, including most cases of Philadelphia chromosome-positive chronic myelogenous leukemia. Oligomerization of Bcr-Abl is essential for oncogenicity. We determined the crystal structure of the N-terminal oligomerization domain of Bcr-Abl (residues 1-72 or Bcr1-72) and found a novel mode of oligomer formation. Two N-shaped monomers dimerize by swapping N-terminal helices and by forming an antiparallel coiled coil between C-terminal helices. Two dimers then stack onto each other to form a tetramer. The Bcr1-72 structure provides a basis for the design of inhibitors of Bcr-Abl transforming activity by disrupting Bcr-Abl oligomerization.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Binding Sites
  • Crystallization
  • Crystallography, X-Ray
  • Dimerization
  • Drug Design
  • Enzyme Activation
  • Enzyme Inhibitors / metabolism
  • Fusion Proteins, bcr-abl / antagonists & inhibitors
  • Fusion Proteins, bcr-abl / chemistry*
  • Fusion Proteins, bcr-abl / genetics
  • Fusion Proteins, bcr-abl / metabolism*
  • Humans
  • Models, Molecular
  • Molecular Sequence Data
  • Mutation / genetics
  • Protein Structure, Quaternary
  • Protein Structure, Tertiary
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Fusion Proteins, bcr-abl

Associated data

  • PDB/1K1F