Anti-HIV polypeptide modified by high molecular weight PEG and preparation method and application thereof

A molecular weight and peptide chain technology, applied in the field of anti-HIV peptides and its preparation, can solve the problems of poor water solubility, less research on macromolecular modification, and short half-life

Active Publication Date: 2020-08-25
INST OF MICROBIOLOGY - CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] C34 molecules are used as the first generation of fusion inhibitors, which have problems such as poor water solubility and short half-life. Many scholars have modified C34 molecules with various groups to improve these problems, but there are few studies on macromolecular modifications.

Method used

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  • Anti-HIV polypeptide modified by high molecular weight PEG and preparation method and application thereof
  • Anti-HIV polypeptide modified by high molecular weight PEG and preparation method and application thereof
  • Anti-HIV polypeptide modified by high molecular weight PEG and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0150] Embodiment 1: PEGylated polypeptide PEG 10k Preparation of NC

[0151] At room temperature, 10mg (0.005mmol) mPEG 10k The mixture of Mal and 10 mg (0.0025 mmol) of polypeptide C34NC was dissolved in 10 mL of sodium dihydrogen phosphate / disodium hydrogen phosphate buffer solution (50 mM, pH 8.0-9.0), and the reaction was monitored by HPLC until the reaction of polypeptide C34NC was complete.

[0152] The obtained PEG-modified polypeptide was purified by Agilent 1200 reversed-phase high-performance liquid chromatography. Chromatographic column model: Angilent Eclipse XDB-C8 Semi-Prep, 5μm, 9.4×250mm; eluent composition: mobile phase A (aqueous solution containing 0.1% trifluoroacetic acid by volume), mobile phase B (including volume The percentage concentration is 0.1% trifluoroacetic acid in acetonitrile solution); elution conditions: A linear gradient elution from 40% to 70%, time 11min, elution flow rate 2mL / min, ultraviolet detection wavelength 220nm. Collect the p...

Embodiment 2

[0156] Example 2: PEGylated Polypeptide PEG 20k Preparation of NC

[0157] Except mPEG in embodiment 1 10k Mal to mPEG 20k Besides Mal, prepare, purify and characterize according to the method in embodiment 1, obtain PEG 20k NC (purity is 97.5%), mass spectrometry results are as figure 2 shown.

[0158] Obtained PEG 20k The structure of NC is:

[0159]

Embodiment 3

[0160] Example 3: PEGylated Polypeptide PEG 40k Preparation of NC

[0161] Except mPEG in embodiment 1 10k Mal to mPEG 40k Besides Mal, prepare, purify and characterize according to the method in embodiment 1, obtain PEG 40k NC (purity is 98%), mass spectrometry results are as image 3 shown.

[0162] Obtained PEG 40k The structure of NC is:

[0163]

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Abstract

The present invention relates to PEG modified anti-HIV polypeptides. Specifically, cysteine is added to the N terminal, the C terminal or the 10th position of the C34 polypeptide, a polyethylene glycol group with maleic amide modification is coupled to the cysteine through Michael addition reaction, PEGylation modification is performed on the C34 polypeptide, the molecular weight of a PEG part is10000 or above, preferably 10000 to 100000 DEG C, and more preferably 10000 to 50000 DEG C. The modified C34 peptide has obviously increased water solubility and rat plasma half-life period, is easierto enter lymph nodes and has stronger anti-HIV virus activity on rhesus monkeys which are acutely infected with SHIVSF162P3. The invention also relates to a preparation method and application of thePEG modified anti-HIV polypeptide.

Description

technical field [0001] The invention belongs to the field of biopharmaceuticals, and relates to polyethylene glycol (PEG) modified anti-HIV polypeptides, a preparation method and application thereof. Background technique [0002] AIDS is a disease with a very high fatality rate caused by human immunodeficiency virus (HIV) infection. HIV can cause serious damage to the systemic immune system and pose a great threat to human life and health. Since it was first discovered in 1981, its control has not been effectively solved. At present, AIDS has shown an explosive trend in the world, and the number of HIV carriers in the world has reached about 34 million. According to statistics and estimates from the Ministry of Health of my country, by the end of 2011, the number of living HIV carriers and AIDS patients (PLHIV) in China had reached 780,000 (620,000 to 940,000). Due to the high mutation rate of the virus, no effective cure for AIDS has yet been found. [0003] Most of the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/16C07K1/107A61K38/16A61K47/60A61P31/18
CPCC07K14/005A61K38/162A61K47/60A61P31/18C12N2740/16122
Inventor 李学兵程水红李明莉马丽英
Owner INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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