Activation of the PKC‐isotypes α, β1, γ, δ, and ε by phorbol esters of different biological activities

FEBS Letters

Evans, A.T.²  Olivier, A.R.¹  Evans, F.J.²  Parker, P.J.¹  Ryves, W.J.² 

[1] Imperial Cancer Research Fund, 44 Lincoln's Inn Fields, London WC2A 3PX, UK;Department of Pharmacognosy, The School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX, UK

关键词: Protein kinase C;    Isotype α;    β1;    γ;    δ and ε;    Phorbol ester;    Daphnane ester;    Selective activation;    Ca2+ requirement;    TPA;    tetradecanoylphorbolacetate;    SAPA;    sapintoxin A;    12-O-2-methylaminobenzoyl-13-O-acetyl-4-deoxyphorbol;    DOPP;    12-deoxyphorbol-13-O-phenylacetate;    DOPPA;    12-deoxyphorbol-13-O-phenylacetate-20-acetate Tx;    thymeleatoxin;    9;    13;    14-orthobenzoyl-6-7;    epoxy-resinferonol-12-O-cinnamate;    Rx;    resiniferatoxin;    9;    13;    14-orthophenylacetyl-resiniferonol-20-O-homovanillate;    PKC;    protein kinase C;    PS;    phosphatidylserine;    DAG;    diacylglycerol;   

DOI  :  10.1016/0014-5793(91)80989-G

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Phorbol esters, tetradecanoylphorbolacetate, sapintoxin-A, 12-deoxyphorbol-phenylacetate, 12-deoxyphorbol-phenylacetate-20-acetate, thymeleatoxin and resiniferatoxin were investigated for their abilities to activate the PKC-isotypes α, β₁, γ, δ and ε. PKC-isotypes were grouped into two classes on the basis of Ca²⁺ requirements for activation by phorbol esters; α, β₁, and γ being Ca²⁺-dependent forms and δ and ε being Ca²⁺-independent. PKC-isotype selective activation by phorbol esters was observed in that SAPA failed to activate PKC-δ up to a concentration of 1000 ng ml⁻¹ and DOPPA only activated PKC-β₁, over the same range of concentrations.

【 授权许可】

Unknown