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Recombinant human interleukin-2 and polyethylene coupling compound

A technology of polyethylene glycol and conjugates, which is applied in the field of conjugates of recombinant human interleukin-2 and polyethylene glycol, and can solve the problems of large loss of biological activity

Inactive Publication Date: 2008-01-16
北京紫辰医药生物技术研究所 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, due to direct modification of the active site or steric hindrance, the biological activity of the modified drug is greatly lost

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1CH 3 O-PEG 5000 -OCH 2 CONH-Gly-CONH-(rhIL-2)(I 1 ) Preparation 1.1 CH 3 O-PEG 5000 -OCH 2 Preparation of COOH

[0021] Add 20.0 g (4 mmol) of monomethoxypolyethanol (MW5000) into a round-bottomed flask equipped with a water separator, add toluene to dissolve, distill, and constantly replenish dry toluene, heat to reflux in an oil bath until no Moisture evaporates. The water separator was removed, and 8 mmol of potassium tert-butoxide was added, and the reaction was carried out under reflux for 1 hour. Then 8 mmol of ethyl bromoacetate was slowly added, and the reaction was refluxed for 6 hours. Filtration, the filtrate was evaporated to dryness under reduced pressure, with CH 2 Cl 2 Dissolve the residue, add anhydrous ether to precipitate a solid, filter the solid, dissolve it in water, slowly add 0.1N sodium hydroxide solution until the pH reaches 10, and stir at room temperature for 2 hours. Then adjust the pH to 3 with 0.1N hydrochloric acid solu...

Embodiment 2

[0027] Example 2CH 3 O-PEG 12000 -OCH 2 CONH-Gly-CONH-(rhIL-2)(I 2 ) preparation

[0028] With reference to the method of Example 1.1, CH 3 O-PEG 12000 -OCH 2 COOH.

[0029] With reference to the method of embodiment 1.2, use CH 3 O-PEG 12000 -OCH 2 COOH instead of CH 3 O-PEG 5000 -OCH 2 COOH to CH 3 O-PEG 12000 -OCH 2 CONH-Gly-COOSu.

[0030] With reference to the method of embodiment 1.3, use CH 3 O-PEG 12000 -OCH 2 CONH-Gly-COOSu instead of CH 3 O-PEG 5000 -OCH 2 CONH-Gly-COOSu, reacts with rhIL-2 to produce CH 3 O-PEG 12000 -CH 2 CONH-Gly-CONH-(rhIL-2).

Embodiment 3

[0031] Example 3CH 3 O-PEG 12000 -OCH 2 CONH-Ala-CONH-(rhIL-2)(I 3 ) preparation

[0032] With reference to the method of Example 2, replace glycine with L-alanine to prepare CH 3 O-PEG 12000 -OCH 2 CONH-Ala-COOSu.

[0033] With reference to the method of embodiment 1.3, use CH 3 O-PEG 12000 -OCH 2 CONH-Ala-COOSu instead of CH 3 O-PEG 5000 -OCH 2 CONH-Gly-COOSu, reacts with rhIL-2 to produce CH 3 O-PEG 12000 -CH 2 CONH-Ala-CONH-(rhIL-2).

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PUM

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Abstract

The invention relates to a coupling compound formed by the recombinant human interleukin-2 connecting with the monomethyl polyethylene glycol through the amino acid or the oligopeptide; the coupling compound has rather good plasma stability, and can release and recompose the recombinant human interleukin slowly to actively play the pharmacological action.

Description

technical field [0001] The present invention relates to a conjugate formed by linking recombinant human interleukin-2 with monomethyl polyethylene glycol through amino acid or oligopeptide; this conjugate has good plasma stability and can slowly release recombinant human interleukin in vivo to exert its pharmacological activity effect. Background technique [0002] Recombinant human interleukin-2 has biological activities such as promoting the maturation and differentiation of T cells, activating lymphokine-activated killer cells, and promoting the production of interferon. It is one of the most important cytokines in immunotherapy and has good clinical antitumor effects. active. [0003] However, as a protein drug, recombinant human interleukin-2 is easily inactivated by enzymatic hydrolysis in the body, and its biological half-life is short, which affects its pharmacological effects. [0004] Polyethylene glycol (PEG) is a neutral polymer with good biocompatibility, high...

Claims

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Application Information

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IPC IPC(8): A61K47/48C07K17/08A61K38/20A61P35/00A61K47/60
Inventor 李广善靳雪峰傅李芳
Owner 北京紫辰医药生物技术研究所
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