Three-dimensional structures and properties of a transforming and a nontransforming glycine-12 mutant of p21H-ras

Biochemistry. 1993 Aug 24;32(33):8411-20. doi: 10.1021/bi00084a005.

Abstract

The three-dimensional structures and biochemical properties of two mutants of the G-domain (residues 1-166) of p21H-ras, p21 (G12D) and p21 (G12P), have been determined in the triphosphate-bound form using guanosine 5'-(beta,gamma-imido)triphosphate (GppNHp). They correspond to the most frequent oncogenic and the only nononcogenic mutation of Gly-12, respectively. The G12D mutation is the only mutant analyzed so far that crystallizes in a space group different from wild type, and the atomic model of the protein shows the most drastic changes of structure around the active site as compared to wild-type p21. This is due to the interactions of the aspartic acid side chain with Tyr-32, Gln-61, and the gamma-phosphate, which result in reduced mobility of these structural elements. The interaction between the carboxylate group of Asp-12 and the gamma-phosphate is mediated by a shared proton, which we show by 31P NMR measurements to exist in solution as well. The structure of p21 (G12P) is remarkably similar to that of wild-type p21 in the active site, including the position of the nucleophilic water. The pyrrolidine ring of Pro-12 points outward and seems to be responsible for the weaker affinity toward GAP (GTPase-activating protein) and the failure of GAP to stimulate GTP hydrolysis.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Base Sequence
  • Binding Sites
  • Circular Dichroism
  • Conserved Sequence
  • GTP Phosphohydrolases / chemistry
  • GTP Phosphohydrolases / metabolism
  • Genes, ras
  • Glycine*
  • Guanosine Triphosphate / metabolism
  • Guanylyl Imidodiphosphate / metabolism
  • Magnesium / metabolism
  • Mammals
  • Models, Molecular
  • Molecular Sequence Data
  • Mutagenesis, Site-Directed
  • Oligodeoxyribonucleotides
  • Point Mutation*
  • Polymerase Chain Reaction / methods
  • Protein Conformation*
  • Proto-Oncogene Proteins p21(ras) / chemistry*
  • Proto-Oncogene Proteins p21(ras) / genetics
  • Proto-Oncogene Proteins p21(ras) / metabolism*
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / isolation & purification
  • Recombinant Proteins / metabolism
  • Thermodynamics

Substances

  • Oligodeoxyribonucleotides
  • Recombinant Proteins
  • Guanylyl Imidodiphosphate
  • Guanosine Triphosphate
  • GTP Phosphohydrolases
  • Proto-Oncogene Proteins p21(ras)
  • Magnesium
  • Glycine