Monomethyl auristatin E, freie Base

Monomethyl auristatin E (MMAE) is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin. MMAE can potentially diffuse into other nearby tumor cells that are antigen negative and be cytotoxic to these cells (bystander killing effect). MMAE is a Tubulin inhibitor. Mode of action: prevent tubulin polymerization. The family of auristatins are synthetic analogues of the antineoplastic natural product Dolastatin 10. MMAE is 100-1000 times more potent than doxorubicin. Bentuximab vedotin is currently the only approved MMAE-conjugate for the treatment of patients with Hodkin lymphoma and anaplatic large cell lymphoma. Some historic facts: The isolation and identification by the Pettit group of dolastatin 10 was reported in 1987. Due to the very low levels of naturally occurring dolastatins, Prof. Pettit, the original discoverer of this highly potent series and collaborators were forced to develop novel synthetic methods in order to obtain enough material to perform even basic cell biology trials. Potential mode of action/Key words: Targeting Tubulin, Antimitotic, Cytotoxic, Anticancer