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Tumor-targeted aptamer drug conjugate

A nucleic acid aptamer and tumor-targeting technology, applied in the field of biomedicine, can solve the problems of high immunogenicity, high cost, and difficult modification, and achieve the effect of prolonging half-life and reducing side effects

Pending Publication Date: 2022-04-26
RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are many problems with antibodies, such as high immunogenicity, high cost, large batch-to-batch variation, difficult modification, low temperature storage and transportation, etc. [7] In comparison, aptamers just solve the above problems [8]

Method used

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Examples

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Effect test

Embodiment 1

[0059] A tumor-targeted nucleic acid aptamer drug conjugate, the nucleic acid aptamer drug conjugate includes a nucleic acid aptamer and a drug, and the chemical formula of the nucleic acid aptamer drug conjugate is:

[0060]

[0061] Those skilled in the art can add or delete several bases at the end (or head) of the sequence according to requirements, and this operation can still achieve the purpose of the present invention and is within the description and protection scope of the present invention.

[0062] The nucleic acid aptamer is correspondingly linked with the drug through a link. The nucleic acid aptamer is covalently coupled to the drug.

[0063] The sulfhydryl group of the nucleic acid aptamer is covalently coupled with the maleamide bond of the drug. The nucleic acid aptamer is a nucleic acid aptamer containing a sulfhydryl group. The terminal of the nucleic acid aptamer is modified with C18 or F base. The sulfhydryl group contained at the end of the nucleic...

Embodiment 2

[0071] A tumor-targeted nucleic acid aptamer drug conjugate, the nucleic acid aptamer drug conjugate includes a nucleic acid aptamer and a drug, and the chemical formula of the nucleic acid aptamer drug conjugate is:

[0072]

[0073] Those skilled in the art can add or delete several bases at the end (or head) of the sequence according to requirements, and this operation can still achieve the purpose of the present invention and is within the description and protection scope of the present invention.

[0074] The difference is that in this example, the nucleic acid aptamer drug conjugate is used for the targeted therapy of colon cancer.

[0075] in, Figure 6 The targeted binding ability of the nucleic acid aptamer-drug conjugates in this example was examined by flow cytometry. 250nM nucleic acid aptamer drug complex or simple nucleic acid aptamer was incubated with colon cancer cell HCT116 in 200ul buffer system for 30 minutes, and the fluorescence on the cell surface wa...

Embodiment 3

[0081] A tumor-targeted nucleic acid aptamer drug conjugate, the nucleic acid aptamer drug conjugate includes a nucleic acid aptamer and a drug, and the chemical formula of the nucleic acid aptamer drug conjugate is:

[0082]

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Abstract

The invention discloses a tumor-targeted nucleic acid aptamer drug conjugate, the nucleic acid aptamer drug conjugate comprises a nucleic acid aptamer and a drug, and the nucleic acid aptamer and the drug are correspondingly connected through a connecting bond. The nucleic acid aptamer is covalently coupled with the medicine. The sulfydryl of the nucleic acid aptamer is correspondingly covalently coupled with the maleic amide bond of the medicine. The nucleic acid aptamer is a nucleic acid aptamer containing sulfydryl. The tail end of the nucleic acid aptamer is modified with C18 or F basic groups. And the medicine is VC-MMAE (Vitamin C-Methyl Methacrylate The aptamer drug conjugate is used for targeted therapy of tumors. According to the tumor-targeted aptamer drug conjugate disclosed by the invention, VC-MMAE is connected to an aptamer with a tumor-targeted effect, so that tumor targeting is realized, and toxic and side effects of drugs are reduced.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a tumor-targeted nucleic acid aptamer drug conjugate. Background technique [0002] Nucleic acid aptamer is a piece of single-stranded DNA or RNA, which is usually obtained by screening (exponential enrichment ligand evolution technique, SELEX), and has strong affinity and specificity for ligands[1,2]. There are currently hundreds of aptamers based on various targets, such as organs, cells, tissues, proteins, small molecules, etc. Among them, there are hundreds of articles based on tumor cells and tumor-related proteins [3]. Among them, the aptamer Ap3 was screened in 2012[4]. At present, many nucleic acid aptamers are in the clinical research stage, but currently only one nucleic acid aptamer targeting VEGF is approved by the FDA for age-related macular degeneration [5]. [0003] MMAE is a highly toxic microtubule inhibitor and cannot be used as a drug alone. It is currently used t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/54A61K31/513A61K31/7068A61K38/07A61P35/00
CPCA61K47/549A61K31/7068A61K38/07A61K31/513A61P35/00
Inventor 谭蔚泓孙洋刘庄肖泽宇
Owner RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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