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dolastatins


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A family of small peptides with diverse activities originally isolated from the marine nudibranch mollusc Dolabella auricularia (sea hare), although they may actually be of cyanobacterial origin. Dolastatin 10 is a potent antimitotic pentapeptide that inhibits microtubule assembly and is being tested in cancer therapy. Dolastatin 11, a depsipeptide, binds to actin and stabilizes F-actin in vitro, like phalloidin and jasplakinolide although acting at a different site. Tasidotin, a synthetic analogue of dolastatin 15, inhibits microtubule assembly and induces a G2/M block in treated tumour-derived cells, ultimately resulting in apoptosis. Lyngbyastatin 4 is a depsipeptide isolated from the marine cyanobacterium Lyngbya confervoides and is an analogue of dolastatin 13; it selectively inhibits elastase and chymotrypsin in vitro. See doliculide; phomopsin A.

Subjects: Medicine and Health.


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