172749-96-1Relevant articles and documents
Use of pyridazinediones as extracellular cleavable linkers through reversible cysteine conjugation
Bahou, Calise,Spears, Richard J.,Aliev, Abil E.,Maruani, Antoine,Fernandez, Marcos,Javaid, Faiza,Szijj, Peter A.,Baker, James R.,Chudasama, Vijay
supporting information, p. 14829 - 14832 (2019/12/24)
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.
A convenient catalyst for aqueous and protein Suzuki-Miyaura cross-coupling
Chalker, Justin M.,Wood, Charlotte S. C.,Davis, Benjamin G.
supporting information; experimental part, p. 16346 - 16347 (2010/01/29)
(Figure Presented) A phosphine-free palladium catalyst for aqueous Suzuki-Miyaura cross-coupling is presented. The catalyst is active enough to mediate hindered, ortho-substituted biaryl couplings but mild enough for use on peptides and proteins. The Suzuki-Miyaura couplings on protein substrates are the first to proceed in useful conversions. Notably, hydrophobic aryl and vinyl groups can be transferred to the protein surface without the aid of organic solvent since the aryl- and vinylboronic acids used in the coupling are water-soluble as borate salts. The convenience and activity of this catalyst prompts use in both general synthesis and bioconjugation.
