Isozyme-specific inhibitors and activators of protein kinase C

Methods Enzymol. 2002;345:470-89. doi: 10.1016/s0076-6879(02)45039-2.

Abstract

We describe here the methods we have used to generate selective peptide inhibitors and activators of PKC-mediated signaling. These approaches should be applicable to any signaling event that is dependent on protein-protein interaction. Furthermore, targeting downstream enzymes in signal transduction has been notoriously difficult as there are often families of related enzymes in each cell. The approaches we have used overcame this difficulty and may prove useful not only in basic research, but also in drug discovery.

Publication types

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

MeSH terms

  • 14-3-3 Proteins
  • Amino Acid Sequence
  • Animals
  • Annexin A1 / chemistry
  • Annexin A1 / genetics
  • Annexin A1 / metabolism
  • Binding Sites
  • Enzyme Activation
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / isolation & purification
  • Enzyme Inhibitors / pharmacology
  • Humans
  • In Vitro Techniques
  • Isoenzymes / antagonists & inhibitors
  • Isoenzymes / chemistry
  • Isoenzymes / genetics
  • Isoenzymes / metabolism
  • Molecular Sequence Data
  • Protein Binding
  • Protein Kinase C / antagonists & inhibitors*
  • Protein Kinase C / chemistry
  • Protein Kinase C / genetics
  • Protein Kinase C / metabolism*
  • Protein Structure, Tertiary
  • Rats
  • Receptors for Activated C Kinase
  • Receptors, Cell Surface / chemistry
  • Receptors, Cell Surface / genetics
  • Receptors, Cell Surface / metabolism
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / genetics
  • Recombinant Proteins / metabolism
  • Sequence Homology, Amino Acid
  • Signal Transduction
  • Tyrosine 3-Monooxygenase / chemistry
  • Tyrosine 3-Monooxygenase / genetics
  • Tyrosine 3-Monooxygenase / metabolism

Substances

  • 14-3-3 Proteins
  • Annexin A1
  • Enzyme Inhibitors
  • Isoenzymes
  • Receptors for Activated C Kinase
  • Receptors, Cell Surface
  • Recombinant Proteins
  • Tyrosine 3-Monooxygenase
  • Protein Kinase C