Use of pyridazinediones as extracellular cleavable linkers through reversible cysteine conjugation†
Calise
Bahou, 
‡a
Richard J.
Spears,
‡a
Antoine
Maruani,
a
Marcos
Fernandez,
a
Faiza
Javaid,
a
Peter A.
Szijj,
a
James R.
Baker
*a
and
Vijay
Chudasama
*ab
‡a
Richard J.
Spears,
‡a
Antoine
Maruani,
a
Marcos
Fernandez,
a
Faiza
Javaid,
a
Peter A.
Szijj,
a
James R.
Baker
*a
and
Vijay
Chudasama
*ab
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.
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