Computational analysis of molecular basis of 1:1 interactions of NRG-1beta wild-type and variants with ErbB3 and ErbB4

Proteins. 2005 Jun 1;59(4):742-56. doi: 10.1002/prot.20443.

Abstract

The neuregulin/ErbB system is a growth factor/receptor cascade that has been proven to be essential in the development of the heart and the sympathetic nervous system. However, the basis of the specificity of ligand-receptor recognition remains to be elucidated. In this study, the structures of NRG-1beta/ErbB3 and NRG-1beta/ErbB4 complexes were modeled based on the available structures of the homologous proteins. The binding free energies of NRG-1beta to ErbB3 and ErbB4 were calculated using the molecular mechanics Poisson-Boltzmann surface area (MM-PBSA) computational method. In addition, computational alanine-scanning mutagenesis was performed in the binding site of NRG-1beta and the difference in the binding free energies between NRG-1beta mutants and the receptors was calculated. The results specify the contribution of each residue at the interaction interfaces to the binding affinity of NRG-1beta with ErbB3 and ErbB4, identifying several important interaction residue pairs that are in agreement with previously acquired experimental data. This indicates that the presented structural models of NRG-1beta/ErbB3 and NRG-1beta/ErbB4 complexes are reliable and could be used to guide future studies, such as performing desirable mutations on NRG-1beta to increase the binding affinity and selectivity to the receptor and discovering new therapeutic agents for the treatment of heart failure.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alanine
  • Amino Acid Substitution
  • Binding Sites
  • Conserved Sequence
  • Epidermal Growth Factor / metabolism
  • ErbB Receptors / chemistry
  • ErbB Receptors / metabolism*
  • Genetic Variation
  • Models, Biological
  • Mutagenesis, Site-Directed
  • Neuregulin-1 / chemistry
  • Neuregulin-1 / genetics
  • Neuregulin-1 / metabolism*
  • Protein Isoforms / chemistry
  • Protein Isoforms / metabolism
  • Receptor, ErbB-3 / chemistry
  • Receptor, ErbB-3 / metabolism*
  • Receptor, ErbB-4
  • Recombinant Proteins / metabolism
  • Solvents

Substances

  • Neuregulin-1
  • Protein Isoforms
  • Recombinant Proteins
  • Solvents
  • neuregulin beta
  • Epidermal Growth Factor
  • ErbB Receptors
  • Receptor, ErbB-3
  • Receptor, ErbB-4
  • Alanine