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Monomethyl auristatin E
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Monomethyl auristatin E : ウィキペディア英語版
Monomethyl auristatin E

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Monomethyl auristatin E (MMAE) is a synthetic antineoplastic agent. Because of its toxicity, it cannot be used as a drug itself; instead, it is linked to a monoclonal antibody (MAB) which directs it to the cancer cells. In International Nonproprietary Names for MMAE-MAB-conjugates, the name vedotin refers to MMAE plus its linking structure to the antibody.〔(Statement on a nonproprietary name adopted by the USAN Council: Vedotin )〕 It is a potent antimitotic drug derived from peptides occurring in marine shell-less mollusc ''Dolabella auricularia'' called dolastatins which show potent activity in preclinical studies, both ''in vitro'' and ''in vivo'', against a range of lymphomas, leukemia and solid tumors. These drugs show potency of up to 200 times that of vinblastine, another antimitotic drug used for Hodgkin lymphoma as well as other types of cancer.
MMAE is actually desmethyl-auristatin E; that is, the N-terminal amino group has only one methyl substituent instead of two as in auristatin E itself.〔
==Mechanism of action==
Monomethyl auristatin E is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin. The linker to the monoclonal antibody is stable in extracellular fluid, but is cleaved by cathepsin once the conjugate has entered a tumour cell, thus activating the antimitotic mechanism.〔(Seattle Genetics: Brentuximab vedotin (SGN-35) )〕
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