Reversible Lysine Modification on Proteins by Using Functionalized Boronic Acids
Copyright policy )Reversible Lysine Modification on Proteins by Using Functionalized Boronic Acids
AbstractIminoboronates have been utilized to successfully install azide and alkyne bioorthogonal functions on proteins, which may then be further reacted with their bioorthogonal counterparts. These constructs were also used to add polyethylene glycol (PEG) to insulin, a modification which has been shown to be reversible in the presence of fructose. Finally, iminoboronates were used to assemble a folic acid/paclitaxel small‐molecule/drug conjugate in situ with an IC50 value of 20.7 nM against NCI‐H460 cancer cells and negligible cytotoxicity against the CRL‐1502 noncancer cells.
- University of Lisbon Portugal
Models, Molecular, Azides, Paclitaxel, Lysine, Proteins, Antineoplastic Agents, Phytogenic, Boronic Acids, Cell Line, Polyethylene Glycols, Folic Acid, Alkynes, Cell Line, Tumor, Neoplasms, Animals, Humans, Insulin, Muramidase, Imines
Models, Molecular, Azides, Paclitaxel, Lysine, Proteins, Antineoplastic Agents, Phytogenic, Boronic Acids, Cell Line, Polyethylene Glycols, Folic Acid, Alkynes, Cell Line, Tumor, Neoplasms, Animals, Humans, Insulin, Muramidase, Imines
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