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Aptamer and new use of derivative thereof

A nucleic acid aptamer and derivative technology, which is applied in the direction of non-active ingredient medical preparations, drug combinations, anti-infectives, etc., can solve difficult chemical modification and transformation, poor stability of antibody conjugates, easy to cause immune reactions, etc. problem, to achieve the effect of low cost, good stability, no immune activity and toxicity

Inactive Publication Date: 2009-09-23
谭蔚泓
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Antibodies used for targeted drug delivery are derived from animals or fused monoclonal cells. Poor stability and high cost limit its wide application

Method used

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  • Aptamer and new use of derivative thereof
  • Aptamer and new use of derivative thereof
  • Aptamer and new use of derivative thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1, Screening, Optimization and Transformation of Aptamer I and Aptamer II

[0047] Screening process such as figure 1 As shown (cell A is the target cell, cell B is the counter-screened cell, 1 represents the random DNA library, 2 represents the elution step, 3 represents the PCR step, 4 represents the enriched library, 5 represents cloning and sequencing, 6 represents the entry into the next One round of screening, 7 represents the flow cytometric analysis step), as follows:

[0048] 1. Screening, optimization and transformation of CCRF-CEM nucleic acid aptamers in leukemia cells

[0049] (1) Screening of nucleic acid aptamers

[0050] 1. Design and synthesis of random nucleic acid library

[0051] Design and synthesize a random nucleic acid sequence library containing 18 nucleotides at both ends and 52 nucleotides in the middle as follows: 5'-ATA CCA GCT TAT TCA ATT-52-nt-AGA TAG TAA GTG CAA TCT-3'.

[0052] 2. Screening of nucleic acid aptamers

[0053] ...

Embodiment 2

[0104] Embodiment 2, preparation and application of targeted drug

[0105] 1. Preparation of Targeted Drug I

[0106] The preparation process is as figure 2 shown.

[0107] 1. Preparation of doxorubicin 6-maleimide caproyl hydrazone

[0108] Take doxorubicin hydrochloride (5 mg, 8.62 μmol) and EMCH (N-e-(Maleimidocaproic acid) hydrazide, N-e-maleimidocaproic acid hydrazide) (Pierce Biotechnology) (10 mg, 44.4 μmol) dissolved in 4 mL methanol, add 3 μL Trifluoroacetic acid reacted at room temperature in the dark for 24 hours; then concentrated under reduced pressure at room temperature to 0.25 mL, added 2.5 mL of acetonitrile and placed at 4°C for 48 hours for recrystallization; washed the crystals with a methanol-acetonitrile (1:10) mixture, and dried in vacuo to obtain Doxorubicin 6-maleimide caproylhydrazone (2.9 mg, 3.85 μmol).

[0109] 2. Coupling of nucleic acid aptamers and drugs

[0110] Take 300nmol nucleic acid aptamer A modified by the disulfide bond at the 5' ...

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Abstract

The invention discloses an aptamer and a new use of derivative thereof. The new use provided by the invention is application of aptamer and the derivative thereof in preparation of target drugs. The invention further protects the target drugs obtained by coupling the drugs with the aptamer or the derivative thereof. The invention has the advantages of screening and preparing specific aptamer or derivative thereof under the condition of not knowing the molecular transformation of the target cell surface related to the disease, and can simultaneously obtain multiple aptamers or derivatives thereof of molecular related to the cell surface cell; the specificity of the obtained aptamer or derivative thereof is strongly combined with the disease cell; the aptamer or the derivative thereof can be chemically synthesized in large scale and can be easily connected with the drug molecules and has low cost; the molecular weight of the aptamer or the derivative thereof is relatively small without immunologic competence and toxicity; the aptamer or the derivative thereof has good stability; and the formed target drugs are stable. The invention has very high application value.

Description

technical field [0001] The present invention relates to new applications of nucleic acid aptamers and derivatives thereof. Background technique [0002] Traditional tumor chemotherapy drugs often kill normal cells as well as tumor cells due to their low specificity to tumor cells, resulting in strong toxic and side effects. Tumor cell-targeted drug delivery is an effective way to improve the efficacy of tumor therapy and reduce side effects. Conjugating drugs to tumor cell-specific ligands is the main method of targeted drug delivery. For example, drugs are covalently bound to monoclonal antibodies of cell surface tumor markers, and these drug-coupled monoclonal antibodies can selectively bind to tumor tissues, thereby improving the effect of anti-tumor drugs and reducing toxic and side effects. Combining multiple targeted therapeutic drugs with different mechanisms of action can lead to better therapeutic effects. Many of these drugs have achieved good results in preclin...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61P35/00A61P35/02A61P31/00A61P29/00A61K47/54
Inventor 谭蔚泓上官棣华
Owner 谭蔚泓
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