Transduced p16INK4a peptides inhibit hypophosphorylation of the retinoblastoma protein and cell cycle progression prior to activation of Cdk2 complexes in late G1

Cancer Res. 1999 Jun 1;59(11):2577-80.

Abstract

Progression of cells through the G1 phase of the cell cycle requires cyclin D:Cdk4/6 and cyclin E:Cdk2 complexes; however, the duration and ordering of these complexes remain unclear. To address this, we synthesized a peptidyl mimetic of the Cdk4/6 inhibitor, p16INK4a that contained an NH2-terminal TAT protein transduction domain. Transduction of TAT-p16 wild-type peptides into cells resulted in the loss of active, hypophosphorylated pRb and elicited an early G1 cell cycle arrest, provided cyclin E:Cdk2 complexes were inactive. We conclude that cyclin D:Cdk4/6 activity is required for early G1 phase cell cycle progression up to, but not beyond, activation of cyclin E:Cdk2 complexes at the restriction point and is thus nonredundant with cyclin E:Cdk2 in late G1.

Publication types

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

MeSH terms

  • CDC2-CDC28 Kinases*
  • Cell Line
  • Cyclin D
  • Cyclin E / physiology
  • Cyclin-Dependent Kinase 2
  • Cyclin-Dependent Kinase 4
  • Cyclin-Dependent Kinase 6
  • Cyclin-Dependent Kinase Inhibitor p16 / physiology*
  • Cyclin-Dependent Kinases / physiology*
  • Cyclins / physiology*
  • G1 Phase / physiology*
  • Humans
  • Keratinocytes
  • Phosphorylation
  • Protein Serine-Threonine Kinases / physiology*
  • Proto-Oncogene Proteins*
  • Retinoblastoma Protein / metabolism*
  • Transfection

Substances

  • Cyclin D
  • Cyclin E
  • Cyclin-Dependent Kinase Inhibitor p16
  • Cyclins
  • Proto-Oncogene Proteins
  • Retinoblastoma Protein
  • Protein Serine-Threonine Kinases
  • CDC2-CDC28 Kinases
  • CDK2 protein, human
  • CDK4 protein, human
  • CDK6 protein, human
  • Cyclin-Dependent Kinase 2
  • Cyclin-Dependent Kinase 4
  • Cyclin-Dependent Kinase 6
  • Cyclin-Dependent Kinases