A surface on the G protein beta-subunit involved in interactions with adenylyl cyclases

Proc Natl Acad Sci U S A. 1997 Mar 18;94(6):2711-4. doi: 10.1073/pnas.94.6.2711.

Abstract

Receptor activation of heterotrimeric G proteins dissociates G alpha from the G betagamma complex, allowing both to regulate effectors. Little is known about the effector-interaction regions of G betagamma. We had used molecular modeling to dock a peptide encoding the region of residues 956-982 of adenylyl cyclase (AC) 2 onto Gbeta to identify residues on Gbeta that may interact with effectors. Based on predictions from the model, we synthesized peptides encoding sequences of residues 86-105 (Gbeta 86-105) and 115-135 (Gbeta 115-135) from Gbeta. The Gbeta 86-105 peptide inhibited G betagamma stimulation of AC2 and blocked G betagamma inhibition of AC1 and by itself inhibited calmodulin-stimulated AC1, thus displaying partial agonist activity. Substitution of Met-101 with Asn in this peptide resulted in the loss of both the inhibitory and partial agonist activities. Most activities of the Gbeta 115-135 peptide were similar to those of Gbeta 86-105 but Gbeta 115-135 was less efficacious in blocking G betagamma inhibition of AC1. Substitution of Tyr-124 with Val in the Gbeta 115-135 peptide diminished all of its activities. These results identify the region encoded by amino acids 84-143 of Gbeta as a surface that is involved in transmitting signals to effectors.

Publication types

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

MeSH terms

  • Adenylyl Cyclases / biosynthesis
  • Adenylyl Cyclases / chemistry*
  • Adenylyl Cyclases / metabolism*
  • Amino Acid Sequence
  • Animals
  • Binding Sites
  • Brain / metabolism
  • Cattle
  • GTP-Binding Proteins / biosynthesis
  • GTP-Binding Proteins / chemistry*
  • GTP-Binding Proteins / metabolism*
  • Macromolecular Substances
  • Models, Molecular
  • Peptide Fragments / chemistry
  • Peptide Fragments / pharmacology
  • Protein Biosynthesis
  • Protein Conformation*
  • Protein Structure, Secondary
  • Rabbits
  • Reticulocytes / metabolism

Substances

  • Macromolecular Substances
  • Peptide Fragments
  • GTP-Binding Proteins
  • Adenylyl Cyclases