Phorbolesters enhance basal D-glucose transport but inhibit insulin stimulation of D-glucose transport and insulin binding in isolated rat adipocytes.
The C-kinase activating phorbolester TPA (12-O-Tetradecanoyl-beta-phorbol-13-acetate) and PdBu (4-beta-Phorbol-12,13,dibutyrate) stimulated D-glucose transport twofold in isolated rat adipocytes but inhibited high affinity insulin binding and the responsiveness of D-glucose transport to insulin stimulation by about 30%. Phorbolesters have therefore insulin-like effects but antagonize insulin on receptor and postreceptor level.
Kirsch
D
D
Obermaier
B
B
Häring
H U
HU
D000273:Adipose Tissue / Q000187:drug effects / Q000378:metabolism*; D000818:Animals; D001693:Biological Transport, Active / Q000187:drug effects; D005947:Glucose / Q000378:metabolism*; D007328:Insulin / Q000378:metabolism / Q000494:pharmacology*; D008297:Male; D015240:Phorbol 12,13-Dibutyrate; D010703:Phorbol Esters / Q000494:pharmacology*; D010704:Phorbols / Q000494:pharmacology*; D011493:Protein Kinase C; D011494:Protein Kinases / Q000378:metabolism; D011505:Protein-Tyrosine Kinases; D051381:Rats; D011919:Rats, Inbred Strains; D011972:Receptor, Insulin / Q000378:metabolism; D013755:Tetradecanoylphorbol Acetate / Q000494:pharmacology*
D007328:Insulin; D010703:Phorbol Esters; D010704:Phorbols; D015240:Phorbol 12,13-Dibutyrate; D011494:Protein Kinases; D011505:Protein-Tyrosine Kinases; D011972:Receptor, Insulin; D011493:Protein Kinase C; D005947:Glucose; D013755:Tetradecanoylphorbol Acetate