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Cancer cell-targeting structural molecule and use thereof

A targeting and cancer cell technology, applied in the field of biomedicine, can solve problems such as poor targeting and difficult preparation, and achieve the effect of increasing stability

Inactive Publication Date: 2013-08-07
WUHAN ZEZHI BIOLOGICAL PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The bottleneck problem of effectively exerting the curative effect of siRNA molecules in vivo: the key technology that limits the clinical application of siRNA is that it can effectively penetrate the cell membrane and enter the cytoplasm to play a role in vivo
Current solutions include: cationic liposome and viral vector encapsulation, high-pressure injection, and direct modification of siRNA molecules (such as chemical, lipid, steroid, antibody-protamine, polymer, etc.), but these The method also has defects such as difficult preparation or poor targeting

Method used

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  • Cancer cell-targeting structural molecule and use thereof
  • Cancer cell-targeting structural molecule and use thereof
  • Cancer cell-targeting structural molecule and use thereof

Examples

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Comparison scheme
Effect test

Embodiment 1

[0064] 1. Synthesis of RGD-PEG-MPA-siRNA VEGFR2 molecule.

[0065] Synthetic route such as figure 1 As shown, the specific steps are as follows:

[0066] 1.1. RGD-PEG-MPA (Tumor Targeting Structural Molecule)

[0067] The synthetic steps of RGD-PEG-MPA are as follows figure 1 Shown, it is composed of the oligopeptide cyclo(-Arg-Gly-Asp-D-Phe-Lys-( figure 1 The amino group on Lys in A) is related to 8-amino-3,6-dioxa-octanoic acid ( figure 1 In B, the carboxyl group of PEG) is dehydrated and condensed to obtain RGD-PEG ( figure 1 C in C), then the amino group of RGD-PEG is combined with 3-Maleimidopropionic Acid ( MPA for short, figure 1 The carboxyl group in D) is dehydrated and condensed to obtain RGD-PEG-MPA ( figure 1 E in the tumor-targeting structural molecule). The specific synthesis of RGD-PEG-MPA was entrusted to Peptide International Company of the United States (with a confidentiality agreement signed). Its identification and purification as figure 2 A-C....

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Abstract

The invention discloses a cancer cell-targeting structural molecule and a use thereof. A molecule shown in the formula (I) reacts with a connection molecule containing a carboxyl structure and a maleimide group so that the cancer cell-targeting structural molecule is produced by a dehydration synthesis reaction of an amino group and a carboxyl group. The cancer cell-targeting structural molecule can be bonded with a sulfydryl (-SH)-modified nucleotide molecule, can be directly applied to a human body by blood vessel administration, can be specifically bonded with cancer cells expressing integrin family alpha v beta 3 acceptors or with new vessel endothelial cells in cancer tissue, can effectively penetrate a cell membrane by receptor-mediated endocytosis, and can convey the nucleotide molecule into cytoplasm. In the formula (I), n is in a range of 1-10.

Description

Technical field: [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a cancer cell targeting structural molecule and its application. Background technique: [0002] Since small interfering RNA (siRNA) molecules can inhibit the function of specific target proteins by silencing the expression of target mRNA, the use of siRNAs is expected to become a new therapeutic strategy for a variety of diseases caused by gene mutation or overexpression (Davidson BL, McCray PB Jr. Current prospects for RNA interference-based therapies. Nat Rev Genet. 2011;12(5):329-40). However, the lack of an effective delivery system limits the clinical application of siRNA molecules into target cells. Recently, optimized design and chemical modification have significantly reduced the immune response of siRNA molecules, reduced off-target effects, and increased stability to nucleolisidases (D.V.Morrissey, J.A.Lockridge, L.Shaw, K.Blanchard, K.Jensen , W. Bre...

Claims

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Application Information

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IPC IPC(8): C07K7/64A61K47/48A61K48/00A61P35/00A61K47/59
Inventor 季爱民裘志勇
Owner WUHAN ZEZHI BIOLOGICAL PHARMA
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