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Issue 98, 2019
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Use of pyridazinediones as extracellular cleavable linkers through reversible cysteine conjugation

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Abstract

Herein we report a retro-Michael deconjugation pathway of thiol–pyridazinedione linked protein bioconjugates to provide a novel cleavable linker technology. We demonstrate that the novel pyridazinedione linker does not suffer from off-target modification with blood thiols (e.g., glutathione, human serum albumin (HSA)), which is in sharp contrast to an analogous maleimide linker.

Graphical abstract: Use of pyridazinediones as extracellular cleavable linkers through reversible cysteine conjugation

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Publication details

The article was received on 25 Oct 2019, accepted on 15 Nov 2019 and first published on 18 Nov 2019


Article type: Communication
DOI: 10.1039/C9CC08362F
Chem. Commun., 2019,55, 14829-14832
  • Open access: Creative Commons BY license
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    Use of pyridazinediones as extracellular cleavable linkers through reversible cysteine conjugation

    C. Bahou, R. J. Spears, A. E. Aliev, A. Maruani, M. Fernandez, F. Javaid, P. A. Szijj, J. R. Baker and V. Chudasama, Chem. Commun., 2019, 55, 14829
    DOI: 10.1039/C9CC08362F

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