Format

Send to

Choose Destination
See comment in PubMed Commons below
Chem Commun (Camb). 2013 Sep 25;49(74):8187-9. doi: 10.1039/c3cc45220d.

Acid-cleavable thiomaleamic acid linker for homogeneous antibody-drug conjugation.

Author information

1
Department of Chemistry, University College London, 20 Gordon Street, London, WC1H 0AJ, UK.

Abstract

In this communication we describe a novel acid-cleavable linker strategy for antibody-drug conjugation. Functional disulfide bridging of the single interchain disulfide bond of a trastuzumab Fab fragment yields a homogeneous antibody-drug conjugate bearing a thiomaleamic acid linker. This linker is stable at physiological pH and temperature, but quantitatively cleaves at lysosomal pH to release the drug payload.

PMID:
23929130
PMCID:
PMC3763782
DOI:
10.1039/c3cc45220d
[Indexed for MEDLINE]
Free PMC Article
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Royal Society of Chemistry Icon for PubMed Central
    Loading ...
    Support Center