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Artificially designed HIV (human immunodeficiency virus)-infection-resisting polypeptide, composition and application

A derivative, L-type technology, applied in the treatment or prevention of related diseases caused by HIV infection, acquired immunodeficiency syndrome, non-physiologically toxic salt, anti-HIV infection polypeptide field, can solve the problem of low bioavailability

Inactive Publication Date: 2013-05-29
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

[0006] Secondly, T20 is easily degraded by protease and has low bioavailability in vivo

Method used

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  • Artificially designed HIV (human immunodeficiency virus)-infection-resisting polypeptide, composition and application
  • Artificially designed HIV (human immunodeficiency virus)-infection-resisting polypeptide, composition and application
  • Artificially designed HIV (human immunodeficiency virus)-infection-resisting polypeptide, composition and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0142] Embodiment 1: the preparation of compound 6

[0143] 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, the amino acid is in L configuration, 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 Flash or high-pressure liquid chromatography (HPLC), and the pure peptide content is >95%. Matrix-assisted laser desorption time-of-flight mass spectrometry (MALDI-TOF-MS) confirmed the molecular weight of the peptide sequence.

[0144] Use CEM automatic microwave peptide synthesizer for peptide synthesis, the synthesis conditions...

Embodiment 2-68

[0155] Embodiment 2-68: Preparation of Compound 1-5, 7-68

[0156] Compounds No. 1-No. 5, No. 7-No. 68 were synthesized according to the method of Example (1), and the amino acids were all in L configuration, but the corresponding amino acid residues were replaced.

Embodiment 69

[0157] Example 69: Inhibition of HIV-1 Biological Activity Detection

[0158] Evaluation of compounds inhibiting HIV-1-mediated cell-cell fusion activity (IC 50 ):

[0159] 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 (MolecularProbes, Inc., Eugene, OR), and then, 50 μl of labeled H9 / HIV-1 was added to each well of a 96-well plate IIIB cells (2×10 5 / ml), and then add 50 μl of different concentrations of test samples (compounds prepared in the tested examples 1-34 and 44-53, two-fold serial dilution from a concentration of 250 μg / ml), and incubate at 37°C for 30min; then each well Add 100ul of MT-2 cells (1×10 6 / ml), incubated at 37°C for 2h. Confused and unfused Calcein-labeled HIV-1 infected MT-2 cells (MT-2 is a commonly used effector cell used in this experiment to simulate HIV-infected target cells, commercially available) with an inverted fluore...

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PUM

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Abstract

The invention belongs to the field of biological medicine, relates to artificially designed HIV (human immunodeficiency virus)-infection-resisting polypeptide, in particular to polypeptide as shown in a formula I of Xa1AAXd1Xe1BB-Xa2AAXd2Xe2BB-Xa3AAXd3Xe3BB-Xa4AAXd4Xe4BB-Xa5AAXd5Xe5BB (formal I), and a derivative, a stereoisomer or physiological-toxicity-free salt thereof. The invention further relates to a pharmaceutical composition containing the polypeptide in the formula I and the derivative, the stereoisomer or the physiological-toxicity-free salt of the polypeptide, and application of the polypeptide in the formula I and the derivative, the stereoisomer or the physiological-toxicity-free salt of the polypeptide to treatment or prevention of related diseases and particular acquired immunodeficiency syndrome (AID) caused by HIV infection.

Description

technical field [0001] The invention belongs to the field of biomedicine, and relates to an artificially designed, non-natural sequence anti-HIV infection polypeptide, in particular, to the polypeptide represented by formula I, its derivatives, its stereoisomers, 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] x a1 AAX d1 x e1 BB-X a2 AAX d2 x e2 BB-X a3 AAX d3 x e3 BB-X a4 AAX d4 x e4 BB-X a5 AAX d5 x e5 BB Formula I. Background technique [0003] AIDS is currently prevalent in the world and poses a serious thre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/00A61K38/16A61P31/18
CPCA61K38/16C07K14/00A61P31/18
Inventor 刘克良史卫国王潮蔡利锋贾启燕王昆郑保华张沙白玉
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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