Determinants for substrate phosphorylation by p21-activated protein kinase (gamma-PAK)

Biochemistry. 1997 Dec 23;36(51):16059-64. doi: 10.1021/bi9717845.

Abstract

gamma-PAK, originally designated PAK I and subsequently identified as a member of the p21-activated protein kinase family, has been shown to have cytostatic properties and to be involved in maintaining cells in a nondividing state [Rooney, R. D., et al., (1996) J. Biol. Chem. 271, 21498-21504]. The determinants for phosphorylation of substrates by gamma-PAK have been identified by examining the kinetics of phosphorylation of a series of synthetic peptides patterned after the sequence KKRKSGL, which is the site phosphorylated by gamma-PAK in the Rous sarcoma virus nucleocapsid protein NC in vivo and in vitro. With these peptides, the recognition sequence for gamma-PAK has been shown to contain two basic amino acids in the -2 and -3 positions, as represented by (K/R)RXS, in which the -2 position is an arginine, the -3 position is an arginine or a lysine, and X can be an acidic, basic, or neutral amino acid. A basic amino acid in the -1 or -4 position improves the rate of phosphorylation by increasing the Vmax and decreasing the Km. An acidic amino acid in the -1 position increases the rate (2.5-fold), as does an acidic residue in the -4 position, although to a lower extent (1.6-fold). Proline in the -1 or +1 position has a deleterious effect and inhibits phosphorylation by gamma-PAK. The substrate requirements of protein kinases that recognize basic amino acids on the N-terminal side of the phosphorylatable residue such as cAMP-dependent protein kinase (PKA) and Ca2+/phospholipid-dependent protein kinase (PKC) have been compared with gamma-PAK using the same peptides. An acidic residue in the -1 position negatively affects PKA and PKC; thus, peptides containing the sequence KRES can be used to identify gamma-PAK.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Avian Sarcoma Viruses / chemistry
  • Kinetics
  • Nucleocapsid / chemistry
  • Nucleocapsid / metabolism
  • Oligopeptides / chemical synthesis
  • Oligopeptides / chemistry
  • Oligopeptides / metabolism*
  • Phosphorylation
  • Protein Serine-Threonine Kinases / metabolism*
  • Proteins / chemistry
  • Proteins / metabolism
  • Rabbits
  • Reticulocytes / enzymology
  • Substrate Specificity
  • p21-Activated Kinases

Substances

  • Oligopeptides
  • Proteins
  • Protein Serine-Threonine Kinases
  • p21-Activated Kinases