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LMP1targeted oligonucleotide and application thereof serving as radiotherapeutic sensitizer

An oligonucleotide and nucleotide technology, applied in the field of oligonucleotides targeting EBV virus LMP1, can solve problems such as treatment failure

Inactive Publication Date: 2010-05-26
CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinically, radiotherapy is the first choice of treatment, but it often fails due to radiotherapy resistance

Method used

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  • LMP1targeted oligonucleotide and application thereof serving as radiotherapeutic sensitizer
  • LMP1targeted oligonucleotide and application thereof serving as radiotherapeutic sensitizer
  • LMP1targeted oligonucleotide and application thereof serving as radiotherapeutic sensitizer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0066] Carrying out the chemical synthesis of a modified deoxyribozyme

[0067] The synthesis process was completed by a computer-controlled ABI synthesizer. Different reaction components are programmed to enter the reaction chamber (reaction column) through different pipes.

[0068] 1. Establishment of solid phase reaction

[0069] The synthesis reaction is carried out in a reaction column containing a covalently attached 3'-butanol-based monomer.

[0070] 2. Chain extension reaction

[0071] Synthesis was performed using Cyano-ethyl-phosphoramidite chemistry. Each monomer contains 2'-O-methyl. Each reaction cycle includes: deprotection of reactive groups; incorporation of new monomers; protection of non-reactive groups; and oxidation conversion of triphosphites to triphosphates. In this process, each cycle introduces a new monomer.

[0072] 3. Deprotection response

[0073] After the last mononucleotide reaction, ammonium hydroxide was used to release the reaction produ...

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PUM

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Abstract

The invention relates to an EBV virus LMP1 targeted oligonucleotide and also relates to application of the oligonucleotide in treatment and radiotherapeutic sensitization of nasopharyngeal darcinoma. The oligonucleotide has the following characteristics that: (1) the oligonucleotide is complementary with an EBV LMP1 gene through the oligonucleotide binding sequence; (2) the oligonucleotide consists of 11-70 ribonucleotides, and the ribonucleotides are connected by organic phosphate bonds from the 5' direction to the 3' direction; (3) the 2' site of ribose has a methoxy-substituted radical; and (4) the 3' end is connected with a butanol radical. The modified oligonucleotides have relatively high enzymolysis resistance and biological activity, and can serve as an effective medicine for treating or assisting to treat nasopharyngeal darcinoma or EBV relevant diseases.

Description

technical field [0001] The present invention relates to an oligonucleotide targeting EBV virus LMP1. [0002] The invention also relates to the application of the oligonucleotide in the treatment of nasopharyngeal carcinoma and radiotherapy sensitization. Background of the invention [0003] Nasopharyngeal carcinoma (nasopharyngeal carcinoma, NPC) is a malignant epithelial cell tumor with differences in ethnic and geographical distribution. The incidence rate in southern Chinese population is more than 100 times higher than that in Caucasian population, at 25-30 / 100,000. NPC is one of the most common malignant tumors in China and Southeast Asia. It occurs in all provinces and cities in China. The southern coastal areas are significantly higher than the northern and inland areas. It occurs at any age, and males are higher than females. It is rare in childhood. -The incidence rate in the 40-year-old age group increased sharply, peaked at the age of 40-60, and gradually decrea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H21/00A61K31/7088A61K48/00A61P35/00
Inventor 曹亚孙仑泉
Owner CENT SOUTH UNIV
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