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A modified anti-HIV polypeptide and its preparation method and use

A peptide chain, expression technology, applied in the field of biopharmaceuticals, can solve problems such as extremely poor water solubility

Active Publication Date: 2022-03-15
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

C34 is an anti-HIV peptide with stronger activity than T20, but its poor water solubility prevents this peptide from becoming a clinical drug

Method used

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  • A modified anti-HIV polypeptide and its preparation method and use
  • A modified anti-HIV polypeptide and its preparation method and use
  • A modified anti-HIV polypeptide and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0156] Embodiment 1: PEGylated polypeptide PEG 2000 CC34 and PEG 5000 Preparation of CC34

[0157] At room temperature, 20mg (0.01mmol) mPEG 2000 Mal and mPEG 5000 The mixture of Mal and 10 mg (0.002 mmol) of peptide CC34 was dissolved in 10 mL of sodium dihydrogen phosphate / disodium hydrogen phosphate buffer solution (5 mM, pH 7.2), and 5 mM Na 2 HPO 4 Solution will mPEG 2000 The pH of the Mal reaction solution was adjusted to 7.2, and the mPEG 5000 The pH value of the Mal reaction solution was adjusted to 8.0, and the reaction was monitored by HPLC until the peptide was completely reacted.

[0158] The obtained modified peptides were purified using an Agilent 1200 reversed-phase high-performance liquid chromatograph. Chromatography column model: Angilent Eclipse XDB-C18Semi-Prep, 5μm, 9.4×250mm. Chromatographic operating conditions: linear gradient elution, the eluent is composed of mobile phase A (acetonitrile solution containing 0.1% trifluoroacetic acid in volume ...

Embodiment 2

[0164] Embodiment 2: PEGylated polypeptide C34CPEG 2000 and C34CPEG 5000 preparation of

[0165] In addition to replacing the polypeptide CC34 in Example 1 with polypeptide C34C, the mPEG 2000 The pH of the Mal reaction solution was adjusted to 9.5, and the mPEG 5000 The pH value of the Mal reaction solution was adjusted to 7.2, prepared, purified and characterized according to the method in Example 1 to obtain C34CPEG 2000 (98.0% purity) and C34CPEG 5000 (purity is 97.2%), mass spectrometry results are as Figure 2A-2B shown.

[0166] The prepared C34CPEG 2000 The structure is:

[0167]

[0168] The prepared C34CPEG 5000 The structure is:

[0169]

Embodiment 3

[0170] Embodiment 3: PEGylated polypeptide C34NCPEG 2000 and C34NCPEG 5000 preparation of

[0171] In addition to replacing the polypeptide CC34 in Example 1 with the polypeptide C34NC, the mPEG 2000 Mal and mPEG 5000 The pH value of the reaction solution of Mal was adjusted to outside 7.2, prepared, purified and characterized according to the method in Example 1 to obtain C34NCPEG 2000 (97.2% pure) and C34NCPEG 5000 (purity is 97.2%), mass spectrometry results are as Figure 3A-3B shown.

[0172] C34NCPEG 2000 The structure is:

[0173]

[0174] C34NCPEG 5000 The structure is:

[0175]

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Abstract

The present invention relates to a modified anti-HIV polypeptide. Specifically, a cysteine ​​is added to the N-terminal, C-terminal or 10th position of the C34 polypeptide, and a maleamide-modified sugar group or a polyethylene glycol group is coupled to the half-cysteine ​​by Michael addition reaction. Cystine, glycosylation modification or PEGylation modification on C34 polypeptide. The modified C34 peptide has significantly increased water solubility and rat plasma half-life, and still has anti-HIV virus activity. The present invention also relates to the preparation method and application of the modified anti-HIV peptide.

Description

technical field [0001] The invention belongs to the field of biopharmaceuticals, and relates to a modified anti-HIV polypeptide and its preparation method and application. Background technique [0002] AIDS is a disease with a very high fatality rate caused by human immunodeficiency virus (HIV) infection, which poses 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. 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 vaccine has yet been found. [0003] Most of the currently marketed HIV therapeutic drugs are some small molecule enzyme inhibitors targeting viral reverse transcriptase, integrase, protease, etc. Due to the ultr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/00A61K38/16A61P31/18
CPCC07K14/00C07K19/00A61P31/18A61K38/00
Inventor 李学兵程水红李明莉马丽英邵一鸣
Owner INST OF MICROBIOLOGY - CHINESE ACAD OF SCI