Cantharidin, another natural toxin that inhibits the activity of serine/threonine protein phosphatases types 1 and 2A.
Cantharidin, a natural toxicant of blister beetles, is a strong inhibitor of protein phosphatases types 1 (PP1) and 2A (PP2A). Like okadaic acid, cantharidin inhibits the activity of the purified catalytic subunit of PP2A (IC50 = 0.16 microM) at a lower concentration than that of PP1 (IC50 = 1.7 microM) and only inhibits the activity of protein phosphatase type 2B (PP2B) at high concentrations. Dose-inhibition studies conducted with whole cell homogenates indicate that cantharidin also inhibits the native forms of these enzymes. Thus, cantharidin, which is economical and readily available, may be useful as an additional probe for studying the functions of serine/threonine protein phosphatases.
Honkanen
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Department of Biochemistry, College of Medicine, University of South Alabama, Mobile 36688.
D000818:Animals; D002193:Cantharidin / Q000494:pharmacology*; D002413:Cations, Divalent; D002417:Cattle; D004988:Ethers, Cyclic / Q000494:pharmacology; D019319:Okadaic Acid; D016716:PC12 Cells; D010749:Phosphoprotein Phosphatases / Q000037:antagonists & inhibitors* / Q000145:classification; D010766:Phosphorylation; D011817:Rabbits
D002413:Cations, Divalent; D004988:Ethers, Cyclic; D019319:Okadaic Acid; D010749:Phosphoprotein Phosphatases; D002193:Cantharidin