THIOL-SELECTIVE WATER-SOLUBLE POLYMER DERIVATIVES

摘要

The present invention provides water-soluble, polymer derivatives having a thiol-selective terminus suitable for selective coupling to thiol groups, such as those contained in the cysteine residues of proteins.

主权项

1. A method for preparing a thiol-selective derivative of a water-soluble polymer, said method comprising the steps of:
(i) providing a water-soluble polymer comprising a water soluble polymer segment (“POLY”) having one terminus activated with an electrophile (“-E”), and (ii) reacting said polymer with a molecule comprising a nucleophile (“-NU”) and a thiol-selective moiety selected from the group consisting of thiol, protected thiol, disulfide, maleimide, vinyl sulfone, orthopyridyl disulfide, and iodoacetamide, under conditions effective to promote reaction between said electrophile and said nucleophile to form a polymer product comprising a thiol-selective terminus selected from the group consisting of thiol, protected thiol, disulfide, maleimide, vinyl sulfone, orthopyridyl disulfide and iodoacetamide (“POLY-S”).