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A cyclic pentapeptolide antagonist of ETA and ETB
Aselacin C is a cyclic pentapeptolide antagonist of endothelin receptor type A (ETA) and ETB originally isolated from Acremonium.1 It inhibits the binding of endothelin-1 to isolated bovine atrial membranes and porcine cerebral membranes, which endogenously express high levels of ETA and ETB, respectively, with IC50 values of 60 and 80 µg/ml, respectively.
1.Jackson, M., Burres, N.S., Karwowski, J.P., et al.Aselacins, novel compounds that inhibit binding of endothelin to its receptor. I. The producing organism, fermentation and biological activityJ. Antibiot.47(5)523-527(1994)
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