Target restraint alpha Nu beta3 positive cell proliferation cyclic peptides

A technology of positive cells and cyclic peptides, applied in the field of polypeptide drugs, to achieve the effect of inhibiting cell proliferation

Inactive Publication Date: 2012-05-30
THE THIRD AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIV OF PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the application of this targeting component to introduce NF-κB inhibitors into αvβ3 positive cells has not been reported yet

Method used

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  • Target restraint alpha Nu beta3 positive cell proliferation cyclic peptides
  • Target restraint alpha Nu beta3 positive cell proliferation cyclic peptides
  • Target restraint alpha Nu beta3 positive cell proliferation cyclic peptides

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1, the physicochemical property analysis of polypeptide

[0029] The amino acid sequence of the polypeptide molecule of the present invention is input according to the format required by the ANTHPROT V5.0 software, and then various physical and chemical characteristic constants of the polypeptide molecule are calculated.

[0030] The results are shown in Table 1, figure 1

[0031] Table 1 Analysis results of polypeptide physical and chemical characteristic constants

[0032]

Embodiment 2

[0033] Example 2. Competitive inhibition experiments of polypeptides on the binding of nuclear factor-κB p65 subunits to DNA cis-acting elements

[0034] Polypeptide 1 is a linear peptide (RLRWRKC), and polypeptide 2 is a full-length cyclic peptide. The sequences were synthesized by Shanghai Huada Tianyuan Biotechnology Co., Ltd. with a purity of >95%. On a 96-well enzyme-linked plate coated with nuclear factor-κB cis-acting elements (purchased from Mercury TM Add 150 μl / well of transcription factor blocking solution to Transfactor p65 kits, and incubate at room temperature for 15 minutes; discard the transcription factor blocking solution, add 50 μl / well of detection samples diluted with transcription factor blocking solution, and the samples contain 10 ng / μl of p65 standard protein as Positive control, p65 standard protein containing 10ng / μl, add positive peptides at a series concentration at the same time, p65 standard protein containing 10ng / μl, add negative peptides at...

Embodiment 3

[0036] Example 3. Laser Confocal Detection of Cyclic Peptide Entry into αvβ3 Positive Cells

[0037] The cyclic peptides and markers in this experiment were synthesized by Shanghai Huada Tianyuan Biotechnology Co., Ltd. with a purity of >95%. In a cell culture system without lipofection transfection, the fluorescein (rhodamine)-labeled polypeptide (final concentration: 75 μM) was mixed with human umbilical vein endothelial cells, other αvβ3 positive cells (such as human breast cancer cells MDA-MB- 231) were co-cultured for 30 minutes, and co-cultured with αvβ3 negative cells (such as mouse macrophages) for 4 hours, and the results were observed under a confocal laser microscope.

[0038] The results showed that fluorescein-labeled polypeptides could be seen in human umbilical vein endothelial cells and human breast cancer cells MDA-MB-231, but even if the polypeptides were co-cultured with mouse macrophages for 4 hours, only a small amount of many peptides could be seen ente...

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PUM

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Abstract

The invention relates to cyclic peptides for inhibiting the proliferation of alpha v beta 3 positive cells in a target direction and the preparation and application thereof. The cyclic peptide has an amino acid sequence as follows: Cys Arg Gly Asp Val Cit Arg Leu Arg Trp Arg Lys Cys, wherein, Cys at the end of N and Cys at the end of C form a ring through a disulfide bond.

Description

technical field [0001] The present invention relates to a polypeptide drug, in particular to a polypeptide capable of preventing and treating angiogenesis-related diseases, their preparation and application. Background technique [0002] Angiogenesis usually occurs only in situations such as wound healing, female menstrual cycle, pregnancy and fetal growth, but it also occurs in the process of chronic inflammation, tumor invasion and metastasis. Angiogenesis-related diseases that occur under pathological conditions include: various tumors; vascular diseases such as vascular malformation, arteriosclerosis, vascular adhesion, and edematous sclerosis; eye diseases such as neovascularization after corneal transplantation, neovascular glaucoma, and diabetic retinopathy , vascular keratopathy, pterygium, retinal degeneration, retrolentic fibrinosis, granular conjunctivitis; inflammatory diseases such as rheumatoid arthritis, systemic lupus erythematosus, thyroiditis; skin diseases...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/08C07K1/20C07K1/06C07K1/04A61K38/10A61K9/19A61K9/08A61P35/00A61P9/00A61P9/10A61P9/14A61P27/02A61P27/06A61P19/02A61P29/00A61P17/06A61P17/08A61P17/10
Inventor 梁华平李小凤韩健黄宏
Owner THE THIRD AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIV OF PLA
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