A kind of anti-tumor small molecular polypeptide and its application

A small molecule polypeptide, anti-tumor technology, applied in the field of biotechnology and medicine, can solve problems such as large molecular weight

Active Publication Date: 2017-08-25
广州恒宁生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Protein drugs can better block the signal transmission of FGFRs, but protein drugs generally have immunogenicity when injected into the human body due to their large molecular weight

Method used

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  • A kind of anti-tumor small molecular polypeptide and its application
  • A kind of anti-tumor small molecular polypeptide and its application
  • A kind of anti-tumor small molecular polypeptide and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 Design and Synthesis of Small Molecular Peptides and Detection of Antitumor Effects

[0023] (1) Design of small molecule peptides

[0024] The present invention adopts the method of bioinformatics, according to the FGF2-FGFR2 protein binding mode, and based on the FGF2-FGFR2 interaction site, designs small molecular polypeptides, and the key sites on FGF2 that interact with FGFR2 are mainly: Tyr-24, Phe -31, Gln-56, Vla-57, Glu-58, Tyr-73, Val-88, Phe-93, Asn-102, Asn-104, Leu-140, Met-142; key to the interaction with FGF2 on FGFR2 The sites are: Leu-166, Ala-168, Pro-170, Val-249, Arg-251, Asp-283, Val-317, Asn-318, Asp-321. Accerly's protein simulation software Discovery Studio2.5 / 3.5 was used to analyze the binding of FGF2 and its specific binding receptor FGFR2IIIc, and each polypeptide contained 1 to 3 key amino acids on FGF2 that interact with FGFR2, and It is required that the length of the polypeptide just falls into the active pocket of the FGFR2 p...

Embodiment 2

[0040] Example 2: Detection of broad-spectrum anti-tumor properties of small molecule polypeptide P5

[0041] (1) Select the test cell line

[0042]The candidate cell lines are DU145 (prostate cancer cell line), SGC7901 (gastric adenocarcinoma cell line), KYSE30 (human esophageal squamous cell line), and KYSE510 (human esophageal line cell line), all of which were purchased from Shanghai Cell Bank.

[0043] (2) Test method

[0044] The test method is the same as in Example 1, and the logarithmic phase cell lines are DU145, SGC7901, KYSE30, and KYSE510.

[0045] (3) Test results

[0046] Such as figure 2 As shown, P5 has a certain level of inhibition on the proliferation of the above four cell lines, and all of them are concentration-gradient dependent. Except for KYSE510 cells, the inhibition rate of other cells has not reached the maximum efficiency. This experiment shows that the inhibitory rate of P5 to the four cell lines is more obvious for DU145, SGC7901, and KYSE51...

Embodiment 3

[0047] Example 3: Analysis of the binding site of P5 peptide on FGFR2 protein

[0048] (1) Select the test cell line

[0049] The P5 peptide has the greatest effect on the growth and proliferation of the DU145 cell line in inhibiting FGFR2. In the subsequent study of the function and molecular mechanism of the P5 peptide in inhibiting cell proliferation, the target cell line is DU145.

[0050] (2) Test methods and results

[0051] ①Discovery Studio 2.5 software opens the FGF2-FGFR2 protein structure (PDB number: 1EV2), finds the homologous sequence of P5 (53-60 amino acids) on the FGF2 protein, selects the FGFR2 protein, adds a surface layer on the surface of the FGFR2 protein, and selects P5 homologous sequence, change the P5 homologous sequence into CPK mode, such as image 3 structure shown. From the results, it can be seen that amino acids such as (Gln-56, Ala-57, Glu-58, Glu-59) in the homologous sequence of P5 peptide just fall in the D3 domain of FGFR2 protein and ar...

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Abstract

The invention discloses an anti-tumor small molecule polypeptide and its application. The amino acid sequence of the anti-tumor small molecule polypeptide is as follows: LQLQAEER. The anti-tumor small molecule polypeptide can specifically bind to FGFR2, block FGFRs signaling pathway, and achieve anti-tumor effect. Therefore, it can be used to prepare antitumor drugs.

Description

technical field [0001] The invention belongs to the fields of biotechnology and medicine, and in particular relates to an anti-tumor small molecule polypeptide and its application. Background technique [0002] FGFRs (fibroblast growth factor receptors) are abnormally expressed in various tumor tissues: the mutation and abnormal amplification of FGFRs play an important role in the occurrence and development of gynecological tumors, especially breast cancer. For example, over-amplification of FGFR1 and FGFR2 was found in breast cancer, FGFR3 mutation was found in bladder cancer, FGFR3 translocation was found in multiple myeloma, and the survival period of pancreatic cancer patients with high FGFR2 expression was significantly shorter For patients with low expression level, there are gene mutations, overexpression or abnormal expression of FGFR2 in gastric cancer, lung cancer, ovarian cancer and endometrial cancer; After transformation into subtype IIIc, it is often accompani...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06A61K38/08A61P35/00
Inventor 陈小佳洪岸
Owner 广州恒宁生物科技有限公司
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