Contractility and inhibition of protein phosphatases by cantharidin.
1. Cantharidin is a natural defensive toxicant produced by blister beetles. 2. Cantharidin shares structural similarity with highly toxic commercial herbicides (e.g., endothall, endothall anhydride and endothall thioanhydride). 3. Cantharidin inhibits the activity of purified catalytic subunits of serine/threonine protein phosphatases (PP) type 1 and type 2A. 4. Cantharidin increases force of contraction in isolated myocardial and vascular preparations. 5. Cantharidin enhances the phosphorylation state of myocardial and vascular regulatory proteins. 6. Cantharidin is a valuable tool for studying the function of PP in regulatory phosphorylation-dephosphorylation events.
Knapp
J
J
Institut für Pharmakologie und Toxikologie, Westfälische Wilhelms-Universität Münster, Germany.
Bokník
P
P
Huke
S
S
Gombosová
I
I
Linck
B
B
Lüss
H
H
Müller
F U
FU
Müller
T
T
Nacke
P
P
Schmitz
W
W
Vahlensieck
U
U
Neumann
J
J
D000818:Animals; D002193:Cantharidin / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006321:Heart / Q000187:drug effects / Q000502:physiology; D006801:Humans; D009119:Muscle Contraction / Q000187:drug effects; D009124:Muscle Proteins / Q000378:metabolism; D009130:Muscle, Smooth / Q000166:cytology / Q000187:drug effects / Q000378:metabolism / Q000502:physiology; D009200:Myocardial Contraction / Q000187:drug effects; D009206:Myocardium / Q000166:cytology / Q000378:metabolism; D010749:Phosphoprotein Phosphatases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010766:Phosphorylation
D004791:Enzyme Inhibitors; D009124:Muscle Proteins; D010749:Phosphoprotein Phosphatases; D002193:Cantharidin