ADCToxinMonomethylauristatinE(MMAE)

Monomethyl auristatin E (MMAE, vedotin) is a very potent anti-mitotic agent that inhibits cell division by blocking the polymerisation of tubulin. Because of ts super toxicity, it cannot be used as a drug itself. In recent cancer therapy developments, it is linked to a monoclonal antibody (mAb) that recognizes a pecific marker expression in cancer cells and directs MMAE to the cancer cells. The linker linking MMAE to the monoclonal antibody is stable in extracellular fluid, but is cleaved by cathepsin once the antibody-drug-conjugate/ADC has bound to the specific cancer cell antigen and entered the cancer cell, thus releasing the oxic MMAE and activating the potent anti-mitotic mechanism.

Reference:

1. 1. Francisco JA, et al. cAC10-vcMMAE, an anti-CD30-monomethyl auristatin E conjugate with potent and selective antitumor activity. (2003) Blood.102(4):1458-65.
2. 2. Junutula JR, et al. Site-specific conjugation of a cytotoxic drug to an antibody improves the therapeutic index. (2008) Nat Biotechnol. 26(8):925-32.
3. 3. Asundi J, et al. An antibody-drug conjugate targeting the endothelin B receptor for the treatment of melanoma. (2011) Clin Cancer Res.17(5):965-75.
4. 4. Younes A, et al. Results of a Pivotal Phase II Study of Brentuximab Vedotin for Patients With Relapsed or Refractory Hodgkin's Lymphoma. (2012) J Clin Oncol. 30(18):2183-9.
5. 5. http://en.wikipedia.org/wiki/Monomethyl_auristatin_E

Products are for research use only. Not for human use.

产品留言

标题

联系人

联系电话

内容

验证码

点击换一张

注：1.可以使用快捷键Alt+S或Ctrl+Enter发送信息!
2.如有必要,请您留下您的详细联系方式!