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Anti-hepatitis b virus X protein polypeptide drug

A hepatitis B virus and drug technology, applied in the direction of antiviral agents, antineoplastic drugs, drug combinations, etc., to achieve good stability, obvious inhibitory effect, and significant pharmaceutical effects

Active Publication Date: 2015-07-01
TIANJIN TOPTECH BIO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, how to improve the resistance of peptide drugs to degradation without destroying their binding properties, so as to retain the efficacy, is still a big problem that plagues the development of peptide drugs.

Method used

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  • Anti-hepatitis b virus X protein polypeptide drug
  • Anti-hepatitis b virus X protein polypeptide drug
  • Anti-hepatitis b virus X protein polypeptide drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0088] Example 1: Design and preparation of polypeptides

[0089] Synthetic polypeptide functional fragment D-TTK001:

[0090] In the present invention, the amino acid sequence synthesized by artificial synthesis is Gly-D-Ser-D-Ala-D-Val-D-Met-D-Phe-D-Ser-D-Ser-D-Lys-D-Glu- D-type polypeptide of D-Arg-Gly (SEQ ID NO: 1) (hereinafter referred to as D-TTK001). The preparation of the polypeptide adopts a solid-phase synthesis method, such as using an AAPPTECAPex396 polypeptide synthesis instrument (purchased from Hong Kong Universal Analytical and Testing Instrument Co., Ltd.), in a closed explosion-proof glass reactor to make amino acids according to the sequence shown in SEQ ID NO: 1, From C-terminus-carboxyl-terminus to N-terminus-amino-terminus, this refers to the first amino acid sequence added to the amino acid sequence Gly-D-Ser-D-Ala-D-Val-D-Met-D-Phe-D-Ser The amino acid monomer of -D-Ser-D-Lys-D-Glu-D-Arg-Gly is the C-terminal Gly, then D-Arg, then D-Glu, until the la...

Embodiment 2

[0093] A. In vitro binding assay

[0094]The plasmid (pET-30a-HBx) for recombinantly expressing the HBx gene was constructed and preserved by itself (Zhang H, et al. J Biomed Biotechnol doi: 10.1155 / 2009 / 289068), and the method in this document was used to complete the expression and purification of HBx, For in vitro binding assays. Biacore3000 biomacromolecule interaction analyzer (manufactured by GE Healthcare) was used to determine the in vitro binding force between polypeptide D-TTK001 and recombinantly expressed HBx protein. Different concentrations of peptides were injected at a rate of 30 μl / min for 180 seconds. During the dissociation phase, HBS-EP buffer was injected at a rate of 30 μl / min for 900 seconds, followed by injection of 2 needles of 1 mM NaOH at a flow rate of 30 μl / min for 20 seconds to regenerate the chip. All signals were corrected via channel 1 as a control channel. The determination of the binding force was tested twice. In the first test, HBX was i...

Embodiment 3

[0129] Example 3: Experiments on the effectiveness of polypeptides in vivo

[0130] 1. Effect of D-TTK001 on HBV DNA in HBV transgenic mice

[0131] (1) The source and characteristics of HBV transgenic mice Guangzhou Junke Taite Pharmaceutical Technology Co., Ltd.

[0132] HBV transgenic mice were purchased from Guangzhou Junke Taite Pharmaceutical Technology Co., Ltd. The animal model is a transgenic mouse Tg(HBV1.3genome)Swb successfully established and bred by Guangzhou Junke Taite Pharmaceutical Technology Co., Ltd. by microinjection method with high expression replication type 1.3 copies of HBV whole gene. Serum HBsAg and HBeAg can be detected with conventional ELISA kits; 93.93% of positive transgenic mice serum HBV DNA has reached 104-106 copy / ml; liver tissue immunohistochemistry has the expression of HBsAg (cytoplasmic type) and HBcAg (nuclear type). Gender, different ages, and different times of the day had no significant effect on the expression of HBsAg, that is,...

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Abstract

The invention relates to the field of polypeptide drugs and relates to a polypeptide of an anti-hepatitis b virus X protein and applications thereof. Particularly, the invention relates to a polypeptide containing a D-amino acid; the polypeptide has a function of inhibiting a hepatitis B virus X protein (HBx), has an effect of inhibiting the activity of the HBx at molecular level, cellular level and animal level and can inhibit the replication of hepatitis B virus DNA and the expression of associated antigens (such as HBeAg) and further inhibit hepatitis and cirrhosis caused by hepatitis B virus infection and hepatic carcinoma based on cirrhosis. The polypeptide can be widely applied to the prevention and treatment of liver diseases including hepatitis, cirrhosis and hepatic carcinoma caused by hepatitis B virus infection.

Description

technical field [0001] The invention relates to the field of polypeptide medicine, in particular to a polypeptide containing D-type amino acid against hepatitis B virus X protein and its application. Background technique [0002] Liver cancer is one of the malignant tumors that lead to the death of patients. Its malignancy is high. In my country, the death rate of liver cancer is second only to gastric cancer, ranking second in the death rate of malignant tumors in my country. According to statistics, there are 300,000 new cases of liver cancer each year in my country, and 110,000 deaths from liver cancer each year. Hepatitis B virus (HBV) infection can lead to hepatitis, liver cirrhosis, and primary liver cancer. In my country, more than 80% of liver cancer patients are HCC after HBV infection, which can be called post-HBV HCC. [0003] HBV is a DNA virus with a length of about 3.2Kb, and its open reading frame expresses hepatitis B virus surface antigen (HBsAg), hepatitis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08A61K38/10A61P31/20
CPCA61K38/10C07K7/08A61P31/20A61P1/16A61P35/00A61K38/00A61K39/292
Inventor 张晓东叶丽虹
Owner TIANJIN TOPTECH BIO SCI & TECH
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