termsTerm
mc-Val-Cit-PABC
aka valine-citrulline linker, vc-MMAE, mc-VC-PABC
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.
Category
ADC chemistry
Pages like this
not linked directly; found by shared links- TermTubulin inhibitor payloads
Shares Tisotumab vedotin, Telisotuzumab vedotin, MMAE, Disitamab vedotin.
- TermCL2A
Shares Linker (ADC), Bystander effect (ADC), Antibody-drug conjugate (ADC).
- TrialinnovaTV 301 / ENGOT-cx12 / GOG-3057
- TermSMCC (thioether, non-cleavable)
- TermSulfo-SPDB (disulfide)
- TermMaleimidocaproyl (mc), non-cleavable
- TargetTissue factor
- TermAcid-labile hydrazone (AcBut)