The mechanism of inhibition of the cyclin-dependent kinase-2 as revealed by the molecular dynamics study on the complex CDK2 with the peptide substrate HHASPRK

Protein Sci. 2005 Feb;14(2):445-51. doi: 10.1110/ps.04959705. Epub 2005 Jan 4.

Abstract

Molecular dynamics (MD) simulations were used to explain structural details of cyclin-dependent kinase-2 (CDK2) inhibition by phosphorylation at T14 and/or Y15 located in the glycine-rich loop (G-loop). Ten-nanosecond-long simulations of fully active CDK2 in a complex with a short peptide (HHASPRK) substrate and of CDK2 inhibited by phosphorylation of T14 and/or Y15 were produced. The inhibitory phosphorylations at T14 and/or Y15 show namely an ATP misalignment and a G-loop shift (~5 A) causing the opening of the substrate binding box. The biological functions of the G-loop and GxGxxG motif evolutionary conservation in protein kinases are discussed. The position of the ATP gamma-phosphate relative to the phosphorylation site (S/T) of the peptide substrate in the active CDK2 is described and compared with inhibited forms of CDK2. The MD results clearly provide an explanation previously not known as to why a basic residue (R/K) is preferred at the P(2) position in phosphorylated S/T peptide substrates.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate / chemistry
  • Amino Acid Motifs
  • Binding Sites
  • CDC2-CDC28 Kinases / antagonists & inhibitors*
  • CDC2-CDC28 Kinases / chemistry*
  • Cyclin-Dependent Kinase 2
  • Enzyme Inhibitors / chemistry*
  • Humans
  • Ions
  • Magnesium / chemistry
  • Models, Molecular
  • Peptides / chemistry*
  • Phosphates / chemistry
  • Phosphorylation
  • Protein Binding
  • Protein Conformation
  • Protein Structure, Tertiary
  • Software
  • Stereoisomerism
  • Threonine / chemistry
  • Time Factors
  • Tyrosine / chemistry
  • X-Rays

Substances

  • Enzyme Inhibitors
  • Ions
  • Peptides
  • Phosphates
  • Threonine
  • Tyrosine
  • Adenosine Triphosphate
  • CDC2-CDC28 Kinases
  • CDK2 protein, human
  • Cyclin-Dependent Kinase 2
  • Magnesium