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US 8,785,595 B2Granted
Functionalising reagents and their uses
AssigneeGlythera Limited
InventorsAndrew Graham Watts, Terrence Kantner, Amanda Barbara MacKenzie
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AssigneeGlythera Limited
InventorsAndrew Graham Watts, Terrence Kantner, Amanda Barbara MacKenzie
Estimating the term…
Reagents and methods for functionalizing polypeptides with moieties poly (alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalizing reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalizing reagent is covalently linked to a poly (alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly (alkylene glycol) molecule and/or the glycan group.
A method for modifying a polypeptide having at least one reactive thiol group, the method comprising contacting the polypeptide with a functionalising reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent capable of reacting with the at least one thiol group of the polypeptide, wherein the functionalising reagent is covalently linked to a poly (alkylene glycol) molecule or a glycan group, so that the vinyl substituent of the functionalising reagent reacts with the thiol group of the polypeptide, thereby to covalently link the poly (alkylene glycol) molecule or glycan group to the polypeptide through functionalising reagent.
A method which comprises contacting a polypeptide having at least one reactive thiol group with a functionalising reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent capable of reacting with the at least one thiol group of the polypeptide, wherein the functionalising reagent is covalently linked to a poly (alkylene glycol) molecule or a glycan group, so that the vinyl substituent of the functionalising reagent reacts with the thiol group of the polypeptide, thereby to covalently link the poly (alkylene glycol) molecule or glycan group to the polypeptide through functionalising reagent.
Dependencies are inferred from the claim text.