Chemically modified protein with polyethyleneglycol
First Claim
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1. A chemically modified protein with insulin secreting activity which comprises an islet-activating protein produced by bacteria belonging to the genus Bordetella and polyethylene glycol moiety of the formula
where R is a protective group for hydroxyl and l is an integer of about 7 to 700, the polyethylene glycol moiety being bound with a primary amino group of the islet-activating protein.
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Abstract
The chemically modified protein of the present invention has a strong islet-activating activity and is lower in various side effects than non-modified IAP, so that it may be employed as a prevention and therapeutic drug for diabetes.
735 Citations
16 Claims
- 1. A chemically modified protein with insulin secreting activity which comprises an islet-activating protein produced by bacteria belonging to the genus Bordetella and polyethylene glycol moiety of the formula
- space="preserve" listing-type="equation">--O--CH.sub.2 CH.sub.2 O).sub.l R
where R is a protective group for hydroxyl and l is an integer of about 7 to 700, the polyethylene glycol moiety being bound with a primary amino group of the islet-activating protein. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16)
- 5. A chemically modified protein as claimed in claim 4, wherein m is 2.
- 6. A chemically modified protein as claimed in claim 2, wherein the spacer is a group of the formula ##STR7## wherein n is an integer from 1 to 3.
- 7. A chemically modified protein as claimed in claim 6, wherein n is 2.
- 8. A chemically modified protein as claimed in claim 2, wherein the average molecular weight of the polyethylene glycol is 350 to 30000.
- 9. A chemically modified protein as claimed in claim 2, wherein the average molecular weight of the polyethylene glycol is 1900 to 15000.
- 10. A chemically modified protein as claimed in claim 2, wherein the average molecular weight of the polyethylene glycol is 5000.
- 11. A chemically modified protein as claimed in claim 2, wherein the islet-activating protein is bound with 1 to 30 spacers.
- 12. A chemically modified protein as claimed in claim 2, wherein the islet-activating protein is bound with 1 to 10 spacers.
- 13. A chemically modified protein as claimed in claim 2, wherein the modification ratio of the primary amino group is 3 to 80%.
- 14. A chemically modified protein as claimed in claim 2, wherein the modification ratio of the primary amino group is 3 to 40%.
- 15. A chemically modified protein as claimed in claim 2, wherein R is C1-3 alkyl or C1-3 alkanoyl.
- 16. A chemically modified protein as claimed in claim 2, wherein R is methyl.
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Current AssigneeTakeda Chemical Industries, Ltd. (Takeda Pharmaceutical Company Limited)
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Original AssigneeTakeda Chemical Industries, Ltd. (Takeda Pharmaceutical Company Limited)
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InventorsIto, Takashi, Nakagawa, Yasushi
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Primary Examiner(s)Schain, Howard E.
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Application NumberUS07/063,400Time in Patent Office544 DaysField of Search530/399, 530/406, 530/410, 530/397, 424/92US Class Current530/399CPC Class CodesA61K 38/164 from bacteriaC07K 1/1077 by covalent attachment of r...Y02P 20/55 Design of synthesis routes,...
