Intramolecular cooperativity in a protein binding site assessed by combinatorial shotgun scanning mutagenesis

J Mol Biol. 2005 Apr 1;347(3):489-94. doi: 10.1016/j.jmb.2005.01.040.

Abstract

Combinatorial shotgun alanine-scanning was used to assess intramolecular cooperativity in the high affinity site (site 1) of human growth hormone (hGH) for binding to its receptor. A total of 19 side-chains were analyzed and statistically significant data were obtained for 145 of the 171 side-chain pairs. The analysis revealed that 90% of the side-chain pairs exhibited no statistically significant pair interactions, and the remaining 10% of side-chain pairs exhibited only small interactions corresponding to cooperative interaction energies with magnitudes less than 0.4 kcal/mol. The statistical predictions were tested by measuring affinities for purified mutant proteins and were found to be accurate for five of six side-chain pairs tested. The results reveal that hGH site 1 behaves in a highly additive manner and suggest that shotgun scanning should be useful for assessing cooperative effects in other protein-protein interactions.

MeSH terms

  • Binding Sites
  • Human Growth Hormone* / chemistry
  • Human Growth Hormone* / genetics
  • Human Growth Hormone* / metabolism
  • Humans
  • Membrane Proteins* / chemistry
  • Membrane Proteins* / genetics
  • Membrane Proteins* / metabolism
  • Models, Molecular
  • Mutagenesis*
  • Protein Binding
  • Protein Structure, Tertiary

Substances

  • Membrane Proteins
  • delta-hGHR
  • Human Growth Hormone