The structure of VcMMAE is composed of the following functional units:

• MC (maleimidocaproyl): As a thiol-reactive linker, it covalently binds to the thiol group of the antibody cysteine ​​residue through Michael addition to form a stable thioether bond, thereby achieving the coupling of the antibody and the toxin.
• Val-Cit dipeptide linker: It is connected by valine (Val) and citrulline (Cit) through a peptide bond, and can be specifically cleaved by lysosomal proteases (such as cathepsin B) that are highly expressed in the tumor microenvironment, triggering the release of the drug in the target cells.
• PAB (p-aminobenzyloxycarbonyl): As a hydrophobic spacer, it is connected to the dipeptide linker through an ester bond. Its steric hindrance effect can avoid the steric interference of the antibody macromolecule on the degradation process of the linker, ensuring the drug release efficiency.
• MMAE (monomethyl auristatin E): It is a microtubule polymerization inhibitor that blocks cell mitosis by binding to β-tubulin. The allyl ester structure in its molecule is an essential group for cytotoxic activity.

This structural design achieves selective killing of tumor cells through the cascade mechanism of "antibody targeting - enzymatic release - microtubule inhibition".

The answer to this question comes from MCE Technical Support.

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