Glycopegylated granulocyte colony stimulating factor

A - Human Necessities – 61 – K

Patent

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Details

A61K 38/19 (2006.01) C07K 14/535 (2006.01)

Patent

CA 2593682

The present invention provides conjugates between Granulocyte Colony Stimulating Factor and PEG moieties. The conjugates are linked via an intact glycosyl linking group that is interposed between and covalently attached to the peptide and the modifying group. The conjugates are formed from both glycosylated and unglycosylated peptides by the action of a glycosyltransferase. The glycosyltransferase ligates a modified sugar moiety onto either an amino acid or glycosyl residue on the peptide. Also provided are pharmaceutical formulations including the conjugates. Methods for preparing the conjugates are also within the scope of the invention.

La présente invention concerne des conjugués entre un facteur de stimulation de colonie de granulocytes et des fractions PEG. Ces conjugués sont liés via un groupe de liaison glycosyle intact qui est interposé entre le peptide et le groupe modificateur et fixé de manière covalente à ceux-ci. Ces conjugués sont formés à partir de peptides glycosilés et de peptides non glycosylés par l'action d'une glycosyletransférase. La glycosyletransférase ligature une fraction sucre modifiée soit sur un acide aminé, soit sur un résidu glycosyle présent sur le peptide. Cette invention concerne aussi des préparations pharmaceutiques comprenant ces conjuguées et des techniques de préparation de ces conjugués.

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