PEGYLATED INTERLEUKIN-10
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Abstract
Interleukin-10 (IL-10) conjugated via a linker to one or more polyethylene glycol (PEG) molecules at a single amino acid residue of the IL-10, and a method for preparing the same, are provided. The method produces a stable mono-pegylated IL-10, which retains IL-10 activity, where pegylation is selective for the N-terminus on one subunit of IL-10 with little or no formation of monomeric IL-10. The method also provides a substantially homogenous population of mono-PEG-IL-10.
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Citations
20 Claims
- 1. A mono-PEG-IL-10.
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7. A PEG-IL-10 comprising the formula:
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[X—
O(CH2CH2O)n]b-L-NH-IL-10,where X is H or C1-4 alkyl, n is 20 to 2300, b is 1 to 9 and L is a C1-11 alkyl linker moiety which is covalently attached to nitrogen (N) of the alpha amino group at the amino terminus of one IL-10 subunit, provided that when b is greater than 1 the total of n does not exceed 2300. - View Dependent Claims (8)
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11. A process for preparing a mono-PEG-IL-10, comprising the step of:
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reacting IL-10 with an activated PEG-aldehyde linker in the presence of a reducing agent to form the mono-PEG-IL-10, wherein the linker is covalently attached to one amino acid residue of the IL-10. - View Dependent Claims (12, 13, 14, 15, 16, 20)
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17. A process for preparing a mono-PEG-IL-10, comprising the step of:
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reacting IL-10 with an activated PEG-propionaldehyde linker in the presence of sodium cyanoborohydride, wherein the molar ratio of IL-10 to sodium cyanoborohydride is from about 1;
5 to about 1;
15, at a pH of about 6.3 to about 7.5 and a temperature of from 18°
C. to 25°
C. to form the mono-PEG-IL-10,wherein the linker is covalently attached to one amino acid residue of the IL-10. - View Dependent Claims (18, 19)
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Specification