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Derivative and Application of Vascular Endothelial Cell Growth Factor Receptor Antagonist Peptide f56

A technology of growth factor receptor and vascular endothelium, which is applied in the field of derivatives of vascular endothelial cell growth factor receptor antagonist peptide F56, can solve the problems of short half-life and achieve inhibition of tumor growth, tumor cell metastasis, and endothelial cell migration active effect

Active Publication Date: 2021-09-17
BEIJING CANCER HOSPITAL PEKING UNIV CANCER HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, although the polypeptide F56 has shown good anti-angiogenesis and tumor growth and metastasis inhibitory effects in in vivo and in vitro experiments, its half-life is too short, which is an important problem in its clinical application.

Method used

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  • Derivative and Application of Vascular Endothelial Cell Growth Factor Receptor Antagonist Peptide f56
  • Derivative and Application of Vascular Endothelial Cell Growth Factor Receptor Antagonist Peptide f56
  • Derivative and Application of Vascular Endothelial Cell Growth Factor Receptor Antagonist Peptide f56

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1. Preparation and identification of F56 modified peptide

[0047] In this example, polypeptide F56 and F56 amino-terminal modified peptide F56-AM ( figure 1 ), the middle region modified peptide F56-BM ( figure 2 ) and C-terminal modified peptide F56-CM ( image 3 ).

[0048] Modified peptide synthesis raw materials and related reagents and instruments:

[0049] 1. Resin: 2-Chlorotryl Chloride Resin with a degree of substitution of 1.03 mmol / g (Tianjin Nankai Synthetic Technology Co., Ltd.);

[0050] 2. Amino acids: Fmoc-Gly-OH (Chengdu Chengnuo, >99%), Fmoc-Leu-OH (Chengdu Chengnuo, >99%), Fmoc-Tyr(Tbu)-OH (Chengdu Chengnuo, >99%) ), Fmoc-Trp(Boc)-OH (Chengdu Chengnuo, >99%), Fmoc-Glu(OtBu)-OH (Chengdu Chengnuo, >99%), Fmoc-Met-OH (Chengdu Chengnuo, >99%) %), Fmoc-Asp(OtBu)-OH (Chengdu Chengnuo, >99%), Fmoc-Ser(tBu)-OH (Chengdu Chengnuo, >99%), Fmoc-His(Trt)-OH (Chengdu Chengnuo, >99%) promise, >99%);

[0051] 3. Raw materials: Fmoc-Lys(Dde)-OH (Bome B...

Embodiment 2

[0135] Example 2. F56 modified peptide can be combined with human serum albumin in vitro

[0136] In this example, it was confirmed by in vitro experiments that the F56-AM, F56-BM and F56-CM of the present invention prepared according to the method of Example 1 can bind to human serum albumin.

[0137] Experimental steps:

[0138] (1) Prepare 25% human serum albumin (3.79mM) solution: weigh 0.25g human serum albumin into a 1.5mL sterile Eppendorf tube, add 750μL sterile phosphate buffer (100mM NaH 2 PO 4 / Na 2 HPO 4 , pH=7.4), vortex to mix, and make up to 1.0 mL. Do not do sonication.

[0139] (2) Preparation of 10 mM polypeptide F56-AM / F56-BM / F56-CM-dimethyl sulfoxide (DMSO) solution: dissolve the above polypeptide to 10 mM with DMSO.

[0140] (3) Preparation of polypeptide reaction solution: Mix the above two solutions in a volume ratio of 9:1 (human serum albumin:modified peptide) to obtain a reaction solution with a corresponding molar ratio of 3:1.

[0141] (4) Wa...

Embodiment 3

[0151] Example 3. Activity study of F56 modified peptides at different sites

[0152] 1. Endothelial cell tubular structure formation (Tubule Formation) experiment

[0153] In this example, Matrigel was used to simulate the basement membrane of mammalian cells in vitro, and the differences in the formation of three-dimensional tubular structures on the extracellular matrix of human umbilical vein endothelial cells (HUVEC) with different treatments were observed.

[0154] The experimental steps of endothelial cell tubular structure formation:

[0155] (1) Pre-thaw Growth Factor Reduced Matrigel (BD company product number: 356230) on ice at 4°C, and pre-cool the 96-well plate and pipette tips at 4°C.

[0156] (2) Put the 96-well plate on ice, spread 50 μl of Matrigel per well, and incubate at 37°C for 30 minutes.

[0157] (3) HUVEC primary cells were digested, counted, diluted to 10,000 cells / 100 μl with serum-free medium, and added with a final concentration of 0.1% BSA and 2...

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Abstract

The present invention provides a derivative of vascular endothelial cell growth factor receptor antagonistic peptide F56 and its application. The derivative of vascular endothelial cell growth factor receptor antagonistic peptide F56 of the present invention is derived from the vascular endothelial cell growth factor receptor antagonistic peptide F56 A peptide derivative formed by linking the MIPA-AEEA-group on the basis of the structure of . In addition to maintaining F56's ability to antagonize the binding of vascular endothelial growth factor (VEGF) to its receptor 1 (VEGFR1), the peptide derivative has anti-angiogenesis and anti-tumor activities, and its action time is significantly longer than that of polypeptide F56. Angiogenesis and antitumor therapy.

Description

technical field [0001] The present invention relates to a vascular endothelial cell growth factor receptor antagonistic peptide F56 derivative and application, specifically, the present invention relates to a vascular endothelial cell growth factor receptor antagonistic peptide F56 derivative and the derivative of the derivative The preparation method and the application of the derivative in the field of anti-angiogenesis and anti-tumor therapy. Background technique [0002] The growth and metastasis of malignant tumors depend on the formation of new blood vessels. If there is no angiogenesis, the tumor will be in a "dormant" state with a diameter of less than 1.5-2 mm for a long time. The anti-angiogenesis treatment strategy has the characteristics of broad anti-tumor spectrum, not easy to develop drug resistance, and easy to reach the target site. Therefore, this strategy has been considered as one of the most promising methods for tumor treatment. Anti-angiogenic drugs s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K19/00C07K1/107A61K38/08A61K38/10A61P35/00A61P35/04
CPCA61K38/00C07K7/06C07K7/08C07K14/765C07K2319/00
Inventor 寿成超赵传科冯君楠王立新
Owner BEIJING CANCER HOSPITAL PEKING UNIV CANCER HOSPITAL
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