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Anti-HIV (Human Immunodeficiency Virus) infection polypeptide, composition and application

A technology of derivatives and peptide sequences, applied in the field of acquired immunodeficiency syndrome, treatment or prevention of related diseases caused by HIV infection, non-physiological toxicity

Active Publication Date: 2012-01-11
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The design based on natural ligand sequences is reasonable and feasible, but due to the high sensitivity of natural origin sequences to drug resistance mutations, this design has certain limitations

Method used

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  • Anti-HIV (Human Immunodeficiency Virus) infection polypeptide, composition and application
  • Anti-HIV (Human Immunodeficiency Virus) infection polypeptide, composition and application
  • Anti-HIV (Human Immunodeficiency Virus) infection polypeptide, composition and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0114] Embodiment 1: the preparation of compound 1

[0115] A standard Fmoc solid-phase peptide synthesis method was used. All peptide sequences are amidated at the C-terminus and acetylated at the N-terminus. Rink Amide resin is selected, and the peptide chain is extended from the C-terminus to the N-terminus. The condensing agent is HBTU / HOBt / DIEA. The deprotecting agent is piperidine / DMF solution. The lysing agent is trifluoroacetic acid (TFA), and the crude peptide is dissolved in water and then freeze-dried for storage. Separation and purification are carried out by medium-pressure liquid chromatography or high-pressure liquid chromatography (HPLC), and the content of pure peptide is >90%. The molecular weight of the peptide sequence was determined by matrix-assisted laser desorption time-of-flight mass spectrometry (MALDI-TOF-MS).

[0116] The microwave peptide synthesis conditions are as follows:

[0117] Amino acids: 0.2M DMF solution,

[0118] Activator: 0.45M ...

Embodiment 2-34

[0127] Embodiment 2-34: Preparation of compound 2-34

[0128] Compounds No. 2-No. 34 were synthesized according to the method in Example (1), except that the corresponding amino acid residues were replaced. The molecular weights of compounds 2-34 are shown in Table 1 below.

Embodiment 35

[0129] Example 35: Detection of inhibition of HIV-1 biological activity

[0130] 1) Evaluation of compounds inhibiting HIV-1-mediated cell-cell fusion activity (IC 50 )

[0131] Detection of HIV-1-Mediated Cell-Cell Fusion by Stain Transfer Assay: HIV-1 IIIB Infected H9 cells (H9 / HIV-1 IIIB ) was labeled with a fluorescent reagent Calcein-AM (Molecular Probes, Inc., Eugene, OR), and then in a 96-well plate at 37 ° C with or without the test compound and MT-2 cells (ratio = 1:10) Cultivate for 2h. Test compounds were serially diluted two-fold from a concentration of 250 μg / ml. Fused and unfused Calcein-labeled HIV-1 infected cells were counted using an inverted fluorescent microscope (Zeiss, Germany). Calculation IC 50 value.

[0132] 2) ELISA detection compound inhibits gp41 6-HB formation activity (IC 50 )

[0133] Sandwich ELISA method to detect C-peptide inhibition of gp41 6-HB formation activity: the test compound was serially diluted two-fold from the concentrati...

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Abstract

The invention belongs to the field of biomedicines, relates to an anti-HIV (Human Immunodeficiency Virus) infection polypeptide, in particular to a polypeptide shown as a formula IY1-IXb1ELXe1BB-SXb2ELXe2BB-IXb3EXd3Xe3BB-Xa4Xb4EXd4Xe4BB-Y2 and a derivative, stereoisomer or salt without physiological toxicity thereof, and also relates to a medicinal composition comprising the polypeptide shown as the formula I and the derivative, stereoisomer or salt without physiological toxicity thereof and application of the polypeptide shown as the formula I and the derivative, stereoisomer or salt without physiological toxicity thereof to treatment or prevention of related diseases caused by HIV infection, in particular to acquired immunodeficiency syndrome (AIDS).

Description

technical field [0001] The present invention belongs to the field of biomedicine, and relates to a polypeptide for anti-HIV infection, specifically, the polypeptide represented by formula I, its derivative, its stereoisomer, or its non-physiologically toxic salt. The present invention also relates to a pharmaceutical composition containing the above-mentioned polypeptide of formula I, its derivative, its stereoisomer, or its non-physiologically toxic salt, and the formula I polypeptide, its derivative, its stereoisomer, or its Use of the non-physiologically toxic salt in the treatment or prevention of related diseases caused by HIV infection, especially acquired immunodeficiency syndrome (AIDS, namely AIDS). [0002] Y 1 -IX b1 ELX e1 BB-SX b2 ELX e2 BB-IX b3 EX d3 x e3 BB-X a4 x b4 EX d4 x e4 BB-Y 2 Formula I. Background technique [0003] AIDS is currently prevalent in the world and poses a serious threat to human health. Human immunodeficiency virus typ...

Claims

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Application Information

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IPC IPC(8): C07K14/00A61K38/16A61P31/18
CPCC12N2740/16033A61K38/00C07K2319/73C12N2740/16122C07K14/005A61P31/18
Inventor 刘克良姜世勃史卫国贾启燕白玉冯思良蔡利锋王潮张沙姜喜凤
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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