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Structural molecule for affinity and target cell uptake capability of enhanced integrin receptor and application thereof

An integrin receptor, affinity technology, applied in the field of biomedicine, can solve the problems of inability and lack of siRNA uptake and release ability

Active Publication Date: 2017-10-03
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 molecule for affinity and target cell uptake capability of enhanced integrin receptor and application thereof
  • Structural molecule for affinity and target cell uptake capability of enhanced integrin receptor and application thereof
  • Structural molecule for affinity and target cell uptake capability of enhanced integrin receptor and application thereof

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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 affinity and target cell uptake capability of enhanced integrin receptor. The structural molecule has a molecular structure shown in a formula (I); the structural molecule is obtained by carrying out reaction between two cRGD oligopeptides and 6-aminocaproic acid, glutamate oligopeptide or / and arginine oligopeptide, 8-amino-3,6-dioxaoctanoic acid or 3-maleimidopropionic acid and the like to perform dehydration condensation on amino and carboxyl. According to the structural molecule disclosed by the invention, tumor cells expressing an alpha v beta 3 receptor and neovascular endothelial cells can be specially combined, the carried molecules such as nucleotide enter cytoplasm through receptor-mediated endocytic uptake, so that the uptake efficiency of expression cells of the alpha v beta 3 receptor is improved and the release of the carried molecules from a target cytoplasm endosome is promoted, and therefore, the structural molecule can be applied to preparation of targeted therapy drugs or disease diagnosis tracer agents.

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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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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