Cantharidin, another natural toxin that inhibits the activity of serine/threonine protein phosphatases types 1 and 2A
RE Honkanen - FEBS letters, 1993 - Wiley Online Library
FEBS letters, 1993•Wiley Online Library
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 μM) at a lower concentration than that of PPI
(IC50= 1.7 μM) 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 …
types 1 (PP1) and 2A (PP2A). Like okadaic acid, cantharidin inhibits the activity of the
purified catalytic subunit of PP2A (IC50= 0.16 μM) at a lower concentration than that of PPI
(IC50= 1.7 μM) 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 …
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 μM) at a lower concentration than that of PPI (IC50 = 1.7 μM) 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.
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