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Chemical modification method of endostatin and its use

An endostatin, chemical modification technology, applied in chemical instruments and methods, peptide preparation methods, organic chemistry, etc.

Inactive Publication Date: 2007-01-10
NANJING UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] According to the current clinical trial data, the therapeutic dose of rhES is 30mg-40mg per person per day. Such a dose requirement is a great challenge for the production of genetic engineering drugs

Method used

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  • Chemical modification method of endostatin and its use
  • Chemical modification method of endostatin and its use
  • Chemical modification method of endostatin and its use

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Experimental program
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Embodiment Construction

[0029] 1. Preparation of PEG-ES:

[0030] (1) Coupling of PEG and ES

[0031] 100ml ES stock solution (pH4.5, 20mM, HAC / NaAc Buffer, protein content is 1.07mg / ml) adjust the pH to 5.52 with 1M NaAc, add the reducing agent sodium cyanoborohydride NaCNBH 3 To the final concentration of 20mM, add 267.5mg of monomethoxy polyethylene glycol propionaldehyde to make the molar ratio of ES to 1:1. Stir gently at 4℃ for 10 hours, and finally adjust the pH to 4.0 with 100mM HCl. The reaction is to form a PEG-ES modification, and the product is identified by SDS-PAGE. (Attached figure 1 )

[0032] (2) Purification of PEG-ES

[0033] The above reaction product was separated and purified with a CM-Sepharose column (bed volume 15ml) with a KTA chromatograph. After loading the sample, 20mM containing 0.1M, 0.2M, 0.3M, NaCl, pH4.5, HAC / NaAc Buffer for stepwise elution (attached figure 2 ) Collect the eluate containing 0.2M NaCl, which is PEG-ES, and freeze-dry after dialysis to obtain 60 mg.

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Abstract

The invention belongs to the field of bio-pharmaceutical products, which provides a chemical modification method for recombinate human rh-Endostatin ('rh-ES' is called for short) through the way of using mPEG-propionaldehyde to be combined on the fixed point of free amino of N-terminal amino acid of rh-ES. Mono-PEG-rhES is the output material, its purity meet the requirements of biological products. It plays a key role in the hydrolysis resistance of trypsin and chymotrypsin, it can be used as long-acting formulations for its stability for pH and temperature and there is a great perspective in the clinical treatment of cancer.

Description

1. Technical Field [0001] The invention belongs to the technical field of biological product pharmacy 2. Background technology: [0002] Endostatin (ES) is an endogenous neovascularization inhibitor discovered by a research team led by Professor Folkman of Harvard University. It has been identified as the C-terminal fragment of collagen XVIII. It has been shown in in vitro and in vivo experiments. Inhibit the proliferation of activated vascular endothelial cells, inhibit the formation of new blood vessels, inhibit tumor formation and metastasis (Okeilly MS, Boehm T, Folkman J. Cell. 1997, 24, 88, 277-285). At present, recombinant human endostatin (rh-ES) has entered clinical trials in the United States and China. [0003] According to the current clinical trial data, the therapeutic dose of rhES is 30mg-40mg per person per day. Such a dose requirement is a big challenge for the production of genetic engineering drugs. How to prevent the high clearance rate of rhES in the body and...

Claims

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Application Information

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IPC IPC(8): C07K17/02C07K1/107A61K47/48A61K38/17A61P35/00A61K47/60
Inventor 王新昌聂永军陈萌陈钧辉徐根兴荣志刚朱浩文
Owner NANJING UNIV
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