Membrane interactions of mastoparan analogues related to their differential effects on protein kinase C, Na,K‐ATPase and HL60 cells

FEBS Letters

Kuo, J.F.¹  Zheng, Bin¹  Vogler, William R.¹  Kim, Young-Sook¹  Raynor, Robert L.¹ 

[1] Departments of Pharmacology and Medicine (Hematology/Oncology), Emory University School of Medicine, Atlanta, GA 30322, USA

关键词: Mastoparan and analogues;    Protein kinase C: Na;    K-ATPase;    HL60 cell;    MP;    mastoparan;    P-MP;    polistes mastoparan;    TPA;    12-O-tetradecanoylphorbol-13-O-acetate;    PDBu;    phorbol 12;    13-dibutyrate;    PS;    phosphatidylserine;    PKC;    protein kinase C;    PKM;    protein kinase M;    ET-18-OCH3;    1-O-octadecyl-2-O-methyl-3-glycero-3-phosphocholine;    IC50;    concentration causing 50% inhibition;   

DOI  :  10.1016/0014-5793(92)80694-C

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Membrane interactions of tetradecapeptide toxin mastoparan (MP) and analogues (MP-3, MP-X and polistes MP), as indicated by inhibition of various enzymatic and cellular activities, were investigated. MP-3 was found to be the least active in inhibiting protein kinase C (PKC; activated by phosphatidylserine vesicles, synaptosomal membranes or phorbol ester), synaptosomal membrane Na.K-ATPase and proliferation and viability or leukemia HL60 cells. MP-3, however, was as active as others in inhibiting PKC activated by arachidonate monomers and phorbol ester binding. The unique properties or MP-3, the [des-lle-Asn²]- analogue or MP, might be related to its low functional amphiphilicity compared to others and useful in further delineating biological activities associated with or regulated by membranes.

【 授权许可】

Unknown