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The effects of phorbol esters with different biological activities on protein kinase C
Authors:Christine A. Ellis  Susan F. Brooks  Gavin Brooks  A. Tudor Evans  Nicholas Morrice  Fred. J. Evans  Alastair Aitken
Abstract: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. α-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).
Keywords:Tumour-promoting phorbol esters  non-promoting phorbol esters  biological activities  activation of protein kinase C  protein kinase C binding  inhibition of activation and binding
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