Protein kinase inhibitor H-7 increases lipoprotein lipase activity in isolated rat fat pads.
A protein kinase inhibitor, 1-(5-isoquinolinesulfonyl)-2-methylpiperazine (H-7) increased lipoprotein lipase (LPL) activity in isolated rat fat pads in a time- and dose-dependent manner. The incubation of H-7 with partially purified LPL did not affect its activity. Under the marked inhibition of protein synthesis by cycloheximide, H-7 still showed a full effect on the increase in LPL activity. A slight but significant increase in LPL activity in the fat pads was observed with inhibitors of cyclic nucleotide-dependent protein kinase. H-7, therefore, may increase LPL activity through processes other than the direct activation of the LPL molecule, or the stimulation of LPL molecule synthesis; probably through a decrease in the activity of protein kinases, especially protein kinase C.
Morita
T
T
Department of Biochemistry, Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University, Japan.
Tsuruzono
Y
Y
Ueki
H
H
D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine; D000273:Adipose Tissue / Q000187:drug effects / Q000201:enzymology*; D000818:Animals; D007546:Isoquinolines / Q000494:pharmacology*; D008071:Lipoprotein Lipase / Q000187:drug effects* / Q000378:metabolism; D008297:Male; D010879:Piperazines / Q000494:pharmacology*; D047428:Protein Kinase Inhibitors; D051381:Rats; D011919:Rats, Inbred Strains
D007546:Isoquinolines; D010879:Piperazines; D047428:Protein Kinase Inhibitors; D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine; D008071:Lipoprotein Lipase