10. (4+2 points) The structure of the anti-tumor agent mertansine (DM1) is given
ID: 206145 • Letter: 1
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10. (4+2 points) The structure of the anti-tumor agent mertansine (DM1) is given as follows: OH H SH CI Mertansine can be covalently linked with the monoclonal antibody Trastuzumab (herceptin) to generate an antibody-drug conjugate (ADC) for treating breast cancer. How would you conjugate mertansine to Trastuzumab using a linker? (Note this is a hypothetical question and there may be several possible answers. Please explain your linker choice and rationale using concepts we have learned in class. Be sure to include the chemical structures) What role is Trastuzumab playing in this ADC? a. b.Explanation / Answer
Mertansine refers to the thiol-containing maytansinoid, DM1 (N2’-deacetyl-N2’-(3-mercapto-1-oxopropyl)maytansine) attached to a monoclonal antibody through reaction of the thiol group with the SPP (N-succinimidyl 4-(2-pyridyldithio)) linker to create an antibody-drug conjugate or ADC.Trastuzumab emtansine (T-DM1) is an anti-HER2/neu antibody-drug conjugate.
Trastuzumab emtansine is a tumor-activated prodrug resulting from the conjugation of the humanized anti-HER2 mAb trastuzumab, which has been used in the treatment of breast cancer , with ImmunoGen Inc's cytotoxic and antimitotic maytansine derivative DM1. The maytansinoids bind microtubules maytansinoids have been recognized to be 20- to 100-fold more potent at blocking mitosis
Trastuzumab is a monoclonal antibody used in breast cancer. Trastuzumab targets the human epidermal growth factor receptor 2 (HER2) receptor on breast cancer cells that express tyrosine kinase receptor. These cancers known as HER2-positive breast cancer. The original studies of trastuzumab showed improved survival in metastatic breast cancer. Antibody–drug conjugates are used to target high-dose chemotherapy directly to the cancer cells. Trastuzumab is used to target this potent chemotherapy agent directly to the HER2-expressing cancer cells
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