Isozyme-specific inhibitors and activators of protein kinase C.
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.
Schechtman
Deborah
D
Department of Molecular Pharmacology, Stanford University School of Medicine, Stanford, California 94305, USA.
Mochly-Rosen
Daria
D
D048948:14-3-3 Proteins; D000595:Amino Acid Sequence; D000818:Animals; D017305:Annexin A1 / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D001665:Binding Sites; D004789:Enzyme Activation; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D008969:Molecular Sequence Data; D011485:Protein Binding; D011493:Protein Kinase C / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D017434:Protein Structure, Tertiary; D051381:Rats; D000075370:Receptors for Activated C Kinase; D011956:Receptors, Cell Surface / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D011994:Recombinant Proteins / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D017386:Sequence Homology, Amino Acid; D015398:Signal Transduction; D014446:Tyrosine 3-Monooxygenase / Q000737:chemistry / Q000235:genetics / Q000378:metabolism
D048948:14-3-3 Proteins; D017305:Annexin A1; D004791:Enzyme Inhibitors; D007527:Isoenzymes; D000075370:Receptors for Activated C Kinase; D011956:Receptors, Cell Surface; D011994:Recombinant Proteins; D014446:Tyrosine 3-Monooxygenase; D011493:Protein Kinase C