US2008113410A1PendingUtilityA1

Method for Rational Pegylation of Proteins

66
Assignee: XENCOR INCPriority: Mar 31, 2003Filed: Oct 30, 2007Published: May 15, 2008
Est. expiryMar 31, 2023(expired)· nominal 20-yr term from priority
Inventors:John DesjarlaisJonathan ZalevskyGregory Moore
G16B 15/20G16B 35/20C07K 1/1077G16B 15/00A61K 47/60C07K 14/535C07K 14/565C07K 2299/00A61K 38/00G16C 20/60C07K 14/61C07K 14/525G16B 35/00C07K 14/505
66
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Claims

Abstract

The present invention relates to the use of simulation technology to rationally optimize the locations and sizes of attached polymeric moieties for modification of therapeutic proteins and the proteins generated from this method.

Claims

exact text as granted — not AI-modified
1 .- 15 . (canceled) 
     
     
         16 . A human G-CSF protein with at least one polymeric moiety attached at at least one amino acid position selected from the group consisting of Gly5, Ala7, Ser 3, Gly27, Glu34, Ala38, Lys41, His44, GlIu46, Glu47, Val49, Leu50, His53, Ser54, Gly56, Trp59, Ser63, Pro66, Ser67, Ala69, Leu70, Gln71, Ala73, Glu94, Pro98, Prol102, Asp105, Thr106, Leu109, Thr116, Gln120, Glul23, Glu124, Gly126, Pro129, Ala130, Leu131, Gln132, Thr134, Gln135, Ala137, Ala140, Ala142, Ser143, Ala144, Phe145, Glu163, Arg167, and Gln174. 
     
     
         17 . The G-CSF protein of  claim 16 , with at least one polymeric moiety attached at least one amino acid position selected from the group consisting of Ala38, Lys41, Glu46, Glu47, Val49, Leu50, His53, Ser54, Gly56, Trp59, Ser63, Pro66, Ser67, Glu94, Pro98, Pro102, Ala130, Leu131, Gln132, Thr134, Gln135, Ala137, Ala140, Ala142, Ser143, Ala144, and Phe145. 
     
     
         18 . The G-CSF protein of  claim 16  wherein at least one attachment sites is selected from the group consisting of Ala38, Glu47, Val49, Ser54, Gly56, Trp59, Pro66, Glu94, Pro102, Gln132, Gln135, Ala144, and Phe145. 
     
     
         19 . The G-CSF protein of  claim 16 , wherein at least one polymeric moiety is attached to a non-natural amino acid. 
     
     
         20 . The G-CSF protein of  claim 19 , wherein at least one polymeric moiety is attached to a p-acetyl-L-phenylalanine. 
     
     
         21 . The G-CSF protein of  claim 16 , wherein at least one polymeric moiety is attached to a cysteine. 
     
     
         22 . The G-CSF protein of  claim 16 , wherein the polymeric moiety is PEG. 
     
     
         23 . The G-CSF protein of  claim 16 , wherein the polymeric moiety is carbohydrate. 
     
     
         24 .- 27 . (canceled)

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