Integrating energy calculations with functional assays to decipher the specificity of G protein-RGS protein interactions

Nat Struct Mol Biol. 2011 Jun 19;18(7):846-53. doi: 10.1038/nsmb.2068.

Abstract

The diverse Regulator of G protein Signaling (RGS) family sets the timing of G protein signaling. To understand how the structure of RGS proteins determines their common ability to inactivate G proteins and their selective G protein recognition, we combined structure-based energy calculations with biochemical measurements of RGS activity. We found a previously unidentified group of variable 'Modulatory' residues that reside at the periphery of the RGS domain-G protein interface and fine-tune G protein recognition. Mutations of Modulatory residues in high-activity RGS proteins impaired RGS function, whereas redesign of low-activity RGS proteins in critical Modulatory positions yielded complete gain of function. Therefore, RGS proteins combine a conserved core interface with peripheral Modulatory residues to selectively optimize G protein recognition and inactivation. Finally, we show that our approach can be extended to analyze interaction specificity across other large protein families.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Binding Sites
  • Colicins / chemistry
  • Colicins / genetics
  • Colicins / metabolism
  • GTP-Binding Proteins / chemistry*
  • GTP-Binding Proteins / metabolism
  • Humans
  • Molecular Sequence Data
  • Mutagenesis, Site-Directed
  • Protein Interaction Domains and Motifs
  • Protein Interaction Mapping
  • Protein Structure, Tertiary
  • RGS Proteins / chemistry*
  • RGS Proteins / genetics
  • RGS Proteins / metabolism
  • Sequence Alignment
  • Structure-Activity Relationship
  • Substrate Specificity

Substances

  • Colicins
  • RGS Proteins
  • GTP-Binding Proteins