cGMP-dependent protein kinase inhibits serum-response element-dependent transcription by inhibiting rho activation and functions

J Biol Chem. 2002 Oct 4;277(40):37382-93. doi: 10.1074/jbc.M204491200. Epub 2002 Jul 15.

Abstract

RhoA, in its active GTP-bound form, stimulates transcription through activation of the serum-response factor (SRF). We found that cGMP inhibited serum-induced Rho.GTP loading and transcriptional activation of SRF-dependent reporter genes in smooth muscle and glial cells in a cGMP-dependent protein kinase (G-kinase)-dependent fashion. Serum stimulation of the SRF target gene vinculin was also blocked by cGMP/G-kinase. G-kinase activation inhibited SRF-dependent transcription induced by upstream RhoA activators including Galpha(13) and p115RhoGEF, with Galpha(13)-induced Rho.GTP loading inhibited by G-kinase. G-kinase had no effect on the high activation levels of RhoA(63L) or the double mutant RhoA(63L,188A) but inhibited transcriptional activation by these two RhoA mutants to a similar extent, suggesting an effect downstream of RhoA and independent of RhoA Ser(188) phosphorylation. Constitutively active forms of the Rho effectors Rho kinase (ROK), PKN, and PRK-2 induced SRF-dependent transcription in a cell type-specific fashion with ROK being the most efficient; G-kinase inhibited transcription induced by all three effectors without affecting ROK catalytic activity. G-kinase had no effect on RhoA(63L)-induced morphological changes in glial cells, suggesting distinct transcriptional and cytoskeletal effectors of RhoA. We conclude that G-kinase inhibits SRF-dependent transcription by interfering with RhoA signaling; G-kinase acts both upstream of RhoA, inhibiting serum- or Galpha(13)-induced Rho activation, and downstream of RhoA, inhibiting steps distal to the Rho targets ROK, PKN, and PRK-2.

Publication types

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

MeSH terms

  • Animals
  • Base Sequence
  • Cattle
  • Coleoptera
  • Cyclic GMP / pharmacology
  • Cyclic GMP-Dependent Protein Kinase Type I
  • Cyclic GMP-Dependent Protein Kinases / genetics
  • Cyclic GMP-Dependent Protein Kinases / metabolism*
  • DNA Primers
  • DNA, Complementary
  • Enzyme Activation / drug effects
  • Gene Expression Regulation
  • Genes, Reporter
  • Genetic Vectors
  • Heart / physiology
  • Humans
  • Luciferases / genetics
  • Pulmonary Artery / physiology
  • Recombinant Fusion Proteins / metabolism
  • Serum Response Element / physiology*
  • Transcription, Genetic* / physiology
  • Vinculin / genetics
  • rhoA GTP-Binding Protein / antagonists & inhibitors*
  • rhoA GTP-Binding Protein / physiology

Substances

  • DNA Primers
  • DNA, Complementary
  • Recombinant Fusion Proteins
  • Vinculin
  • Luciferases
  • Cyclic GMP-Dependent Protein Kinase Type I
  • Cyclic GMP-Dependent Protein Kinases
  • PRKG1 protein, human
  • rhoA GTP-Binding Protein
  • Cyclic GMP