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

K Sugita; D Sawada; M Sodeoka; H Sasai; M Shibasaki

doi:10.1248/cpb.44.463

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.

Authors

K Sugita¹, D Sawada, M Sodeoka, H Sasai, M Shibasaki

Affiliation

¹ Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.

PMID: 8998847
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