The effects of phorbol esters with different activities on protein kinase C

Ellis, C.A., Brooks, S.F., Brooks, G., Evans, A.T., Morrice, N., Evans, F.J. and Aitken, A. (1987) The effects of phorbol esters with different activities on protein kinase C. Phytotherapy Research, 1 (4). 187 -192. ISSN 0951-418X doi: 10.1002/ptr.2650010412

Abstract/Summary

The sapintoxins are a series of naturally occurring fluorescent phorbol esters with a range of selective biological activities (e.g. pro-inflammatory but non-tumour promoting). Their ability to activate protein kinase C (PKC) in vitro has been studied. Both tumour promoting and non-promoting phorbol derivatives activate the enzyme in vitro at low concentrations. 12-deoxyphorbol-13-phenylacetate-20 acetate (DOPPA) acts as a partial agonist in the activation of protein kinase C. Structurally distinct phorbol esters may therefore preferentially activate different forms of protein kinase C. -sapinine, a biologically inactive compound, binds to protein kinase C without stimulating the enzyme and prevents subsequent activation by phorbol esters such as 12-O-tetradecanoyl phorbol-13-acetate (TPA).