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The mc-Val-Cit-PABC linker is the workhorse of the vedotin ADCs: a valine-citrulline dipeptide cut by cathepsin B, releasing MMAE with a bystander effect.
Maleimidocaproyl-valine-citrulline-p-aminobenzylcarbamate links through cysteine thiols, is stable in human plasma, and is cleaved by cathepsins in the lysosome. In mice it is cleaved prematurely by a serum carboxylesterase, which complicated early preclinical testing. Neutropenia is partly attributed to premature release near neutrophil elastase.
Ball-and-stick model from PubChem 2D record (no 3D conformer available). PubChem record
Showing the molecule this term concerns: Enfortumab vedotin.
Shares MMAE, Tisotumab vedotin, Bystander effect (ADC), Telisotuzumab vedotin.
Shares Linker (ADC), Bystander effect (ADC), Antibody-drug conjugate (ADC).
Shares Development of potent monoclonal antibody auristatin conjugates for cancer therapy, Antibody-drug conjugate (ADC).
Shares Telisotuzumab vedotin, Antibody-drug conjugate (ADC).
Shares Telisotuzumab vedotin, Antibody-drug conjugate (ADC).