Membrane interactions of mastoparan analogues related to their differential effects on protein kinase C, Na, K-ATPase and HL60 cells.
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 of 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 of MP-3, the [des-Ile1-Asn2]-analogue of 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.
Raynor
R L
RL
Department of Pharmacology, Emory University School of Medicine, Atlanta, GA 30322.
Kim
Y S
YS
Zheng
B
B
Vogler
W R
WR
Kuo
J F
JF
D000595:Amino Acid Sequence; D000818:Animals; D002455:Cell Division / Q000187:drug effects; D036341:Intercellular Signaling Peptides and Proteins; D008969:Molecular Sequence Data; D010455:Peptides; D015240:Phorbol 12,13-Dibutyrate / Q000378:metabolism; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*; D051381:Rats; D000254:Sodium-Potassium-Exchanging ATPase / Q000037:antagonists & inhibitors*; D013552:Swine; D013570:Synaptic Membranes / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism; D013574:Synaptosomes / Q000187:drug effects / Q000201:enzymology; D014407:Tumor Cells, Cultured; D014862:Wasp Venoms / Q000737:chemistry / Q000494:pharmacology*
D036341:Intercellular Signaling Peptides and Proteins; D010455:Peptides; D014862:Wasp Venoms; D015240:Phorbol 12,13-Dibutyrate; C037500:mastoparan; D011493:Protein Kinase C; D000254:Sodium-Potassium-Exchanging ATPase