The structure of the anti-tumor agent mertansine (DM1) is given as follows: Mert

Question

The structure of the anti-tumor agent mertansine (DM1) is given as follows: 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?

Explanation / Answer

All antibodies contain two functionallly distinct regions called Fab region which specifically bind to antigen and Fc portion, which involed in effector function by binding to cellular receptors. The Fab portion is N terminal side and Fc portion is C-Terminal side, The Fc portion contaion Carboxylic group (COOH). This upon react with The thiol (SH) GROUP OF THE DRUG AND FOR THIO-ESTER BOND AND FINALLY GENERATE ANTIBODY-DRUG CONJUGATE. (ADC). IMMUNO THERAPEUTICS

Antobody - Fc-----------COOH + SH------Drug -----Esterification-----------> Antibody - Fc -------CO-SH-----Drug

Related Questions

Navigate

• Browse (All)
• Browse T
• Subjects

---

---

Integrity-first tutoring: explanations and feedback only — we do not complete graded work. Learn more.