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The effects of phorbol esters with different biological activities on protein kinase C
Author(s) -
Ellis Christine A.,
Brooks Susan F.,
Brooks Gavin,
Tudor Evans A.,
Morrice Nicholas,
Evans Fred. J.,
Aitken Alastair
Publication year - 1987
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.2650010412
Subject(s) - protein kinase c , phorbol , prkcq , biochemistry , enzyme , protein kinase a , in vitro , biological activity , phorbol ester , kinase , chemistry , tetradecanoylphorbol acetate , enzyme inhibitor
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).