The protein kinase C inhibitors Ro 318220 and GF 109203X are equally potent inhibitors of MAPKAP kinase‐1β (Rsk‐2) and p70 S6 kinase

FEBS Letters

Alessi, Dario R¹ 

[1]MRC Protein Phosphorylation Unit, Department of Biochemistry, University of Dundee, Dundee DD1 4HN, UK

关键词: Protein kinase inhibitor;    PKC;    p70 S6 kinase;    Rsk;    PKB;    protein kinase B;    MAP kinase;    mitogen-activated protein kinase;    MAPKK-1;    MAP kinase kinase-1;    MAPKAP-kinase;    MAP kinase-activated protein kinase;    PKA;    cyclic AMP-dependent protein kinase;    PKC;    protein kinase C;   

DOI  :  10.1016/S0014-5793(96)01510-4

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

The protein kinase C (PKC) inhibitors Ro 318220 and GF 109203X have been used in over 350 published studies to investigate the physiological roles of PKC. Here we demonstrate that these inhibitors are not selective for PKC isoforms as was previously assumed. Ro 318220 inhibited MAPKAP kinase-1β (also known as Rsk-2) in vitro (IC₅₀ 3 nM) more potently than it inhibited mixed PKC isoforms (IC₅₀ 5 nM), and it also inhibited p70 S6 kinase (IC₅₀ 15 nM). GF 109203X also potently inhibited MAPKAP kinase-1β (IC₅₀ 50 nM) and p70 S6 kinase (IC₅₀ 100 nM) with similar potency to PKC isoforms (IC₅₀ 30 nM). The inhibition of MAPKAP kinase-1β, p70 S6 kinase, and probably other protein kinases, may explain many of the effects previously attributed to PKC.

【 授权许可】

Unknown