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Structural molecules that enhance integrin receptor affinity and target cell uptake and their applications

A technology of integrin receptors and affinity, applied in the field of biomedicine, can solve the problems of lack, incapacity of siRNA uptake and release ability, etc.

Active Publication Date: 2021-04-06
WUHAN ZEZHI BIOLOGICAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These two patents lack the mechanism of action in the target cell body, and are not capable or too weak for the uptake and release of siRNA, etc.

Method used

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  • Structural molecules that enhance integrin receptor affinity and target cell uptake and their applications
  • Structural molecules that enhance integrin receptor affinity and target cell uptake and their applications
  • Structural molecules that enhance integrin receptor affinity and target cell uptake and their applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Embodiment 1 adopts the following steps:

[0052] 1.1. Synthesize different molecular structures E-2Ahx-[cRGD]2-PEG-MPA (biRGD for short) and E-2R-2Ahx-[cRGD2-PEG-MPA (biRGD2 for short) that enhance the targeting affinity and uptake of tumor sites :

[0053] The synthesis steps of biRGD1 and biRGD2 are as follows: figure 1 and figure 2 As shown, the dehydration condensation of lysine in two monovalent cRGD motifs with 6-aminocaproic acid, glutamic acid and / or arginine, 8-amino-3,6-dioxahexanoic acid affords E-2Ahx -[cRGD]2-PEG or E-2R-2Ahx-[cRGD]2-PEG, then the amino group of PEG is dehydrated and condensed with the carboxyl group of 3-maleimidopropionic acid to obtain E-2Ahx-[cRGD]2 - PEG-MPA and E-2R-2Ahx-[cRGD]2-PEG-MPA.

[0054] 1.2. Synthesis of positive-sense strand RNA with thiol (-SH) modification:

[0055] siACTB is a siRNA molecule that silences human β-actin mRNA and has undergone conventional stability modification; siNC is a siRNA molecule that has no...

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Abstract

The invention discloses a structural molecule for enhancing integrin receptor affinity and target cell uptake ability, which has a molecular structure as shown in formula (I). It is composed of two cRGD oligopeptides with 6-aminocaproic acid, glutamic acid oligopeptide or arginine oligopeptide, 8-amino-3,6-dioxanoic acid or 3-maleimidopropyl It can be obtained by reacting substances such as acids to dehydrate and condense amino groups and carboxyl groups. The structural molecule of the present invention can specifically bind to tumor cells and neovascular endothelial cells expressing αvβ3 receptors, and enter into the cytoplasm through receptor-mediated endocytosis and uptake of molecules such as nucleotides carried by them, thereby increasing the viability of αvβ3 receptor-expressing cells. The uptake efficiency and the promotion of the release of the carried molecules from the target cytoplasmic endosome can be applied to the preparation of targeted therapeutic drugs or tracers for disease diagnosis.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a technology for regulating genes in target cells. Background technique [0002] Small interfering RNA molecules (siRNA) are effector molecules of the RNA interference (RNAi) theory, which can specifically silence genes that cause or promote tumor proliferation, invasion and metastasis, so siRNA molecules, as a new type of cancer treatment candidate drug, have great potential. application potential. [0003] However, siRNA molecules have a large molecular weight and are negatively charged, which are mutually exclusive with the negatively charged and liposoluble properties of the cell membrane. The lack of an effective delivery system makes it difficult to directly enter the cell through the cell membrane, limiting the entry of siRNA molecules. However, the interior of target cells hinders its clinical application. Currently, common siRNA molecule delivery systems for prec...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/64A61K47/66A61P35/00
CPCC07K7/64
Inventor 季爱民岑柏宏
Owner WUHAN ZEZHI BIOLOGICAL PHARMA
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