Ryves W J, Evans A T, Olivier A R, Parker P J, Evans F J
Department of Pharmacognosy, School of Pharmacy, University of London, UK.
FEBS Lett. 1991 Aug 19;288(1-2):5-9. doi: 10.1016/0014-5793(91)80989-g.
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 alpha, beta 1, gamma, delta and epsilon. PKC-isotypes were grouped into two classes on the basis of Ca2+ requirements for activation by phorbol esters; alpha, beta 1, and gamma being Ca(2+)-dependent forms and delta and epsilon being Ca(2+)-independent. PKC-isotype selective activation by phorbol esters was observed in that SAPA failed to activate PKC-delta up to a concentration of 1000 ng.ml-1 and DOPPA only activated PKC-beta 1 over the same range of concentrations.
研究了佛波酯、十四酰佛波醇乙酸酯、沙平毒素-A、12-脱氧佛波醇苯乙酸酯、12-脱氧佛波醇苯乙酸酯-20-乙酸酯、百里香毒素和树脂毒素激活蛋白激酶C（PKC）各亚型α、β1、γ、δ和ε的能力。根据佛波酯激活PKC各亚型对Ca2+的需求，将PKC各亚型分为两类；α、β1和γ是依赖Ca2+的形式，而δ和ε是不依赖Ca2+的形式。观察到佛波酯对PKC各亚型具有选择性激活作用，即沙平毒素-A在浓度高达1000 ng.ml-1时未能激活PKC-δ，而12-脱氧佛波醇苯乙酸酯在相同浓度范围内仅激活PKC-β1。
