Novel phorbol analogs which bind to protein kinase C (PKC) without activation

Chem Pharm Bull (Tokyo). 1996 Feb;44(2):463-5. doi: 10.1248/cpb.44.463.

Abstract

13-Deacetoxy-11-demethyl-phorbol derivatives with acyl groups of various lengths (from hexanoyl to tetradecanoyl) at the C-12 position were synthesized in an optically active form. Although considerable binding affinities to PKC were observed by analogs 3-7, no activation of PKC was seen even at 10 microM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding, Competitive / drug effects
  • Enzyme Activation / drug effects
  • Phorbol 12,13-Dibutyrate / metabolism
  • Phorbol Esters / chemical synthesis
  • Phorbol Esters / metabolism*
  • Protein Binding
  • Protein Kinase C / metabolism*

Substances

  • Phorbol Esters
  • Phorbol 12,13-Dibutyrate
  • Protein Kinase C