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PDGFR-beta gene expression inhibitor and application thereof

A β gene and inhibitor technology, applied in the field of PDGFR-β gene expression inhibitor, can solve the problem that GRPC molecules cannot be used alone, and achieve the effect of inhibiting the expression level

Active Publication Date: 2022-03-08
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, GRPC molecules cannot be used in intracellular research alone, and further modifications are needed to solve the problem of intracellular delivery and improve their resistance to degradation in cells

Method used

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  • PDGFR-beta gene expression inhibitor and application thereof
  • PDGFR-beta gene expression inhibitor and application thereof
  • PDGFR-beta gene expression inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Example 1 Preparation of mPG molecules and mPG-TAT molecules

[0063] 1. Preparation of mPG molecules

[0064] In this example, the porphyrin group was coupled to guanine and a porphyrin-guanine coupling compound was constructed. Porphyrin MPIX is a typical G-quadruplex-specific binding compound, which mainly binds to the terminal plane of the G-quadruplex interaction occurs, the structure of which is as figure 1 Shown is a derivative of the NMM molecule. Using a (PEG)2 linker would be as figure 2 The peptide nucleic acid guanine OGkk containing two D-lysines is ligated with MPIX to obtain image 3 The shown porphyrin-guanine coupling compound (MPIX-(PEG)2-G(PNA)- D- Lys- D- Lys), referred to as mPG. Wherein, the peptide nucleic acid guanine OGkk containing two D-lysines is composed of such as Figure 4 The shown guanine and two D-lysines at the N-terminal of guanine constitute the ESI mass spectrum identification diagram of the peptide nucleic acid guanine OGkk...

Embodiment 2

[0073] Example 2 mPG inhibits the expression level of PDGFR-β gene

[0074] In this example, mPG, mPG-TAT and TMPyP4, a ligand molecule with a classical G-quadruplex structure, were used to treat U2OS cells respectively, and the expression level of PDGFR-β gene was detected by qRT-PCR and Western blot experiments.

[0075] Wherein, the steps of U2OS cell culture include:

[0076] Cells were incubated in DMEM medium supplemented with 10% fetal bovine serum and 100 U / mL penicillin and streptomycin at 37°C, 5% CO 2 conditions, U2OS cells were seeded in 6-well plates (2×10 5 cells / well) and cultured for 12 hours, then added mPG or mPG-TAT with a final concentration of 0, 2, 10 μM and incubated for 48 hours, harvested cells from each culture plate well;

[0077] qRT-PCR quantitative detection steps include:

[0078] Total RNA was extracted from the cells using an RNA extraction kit (Tiangen, China) according to the manufacturer’s instructions, and 1.0 μg of total RNA was reverse...

Embodiment 3

[0083] Example 3 Effects of mPG molecules on the growth of U2OS cells

[0084] In this example, the effects of mPG and mPG-TAT on the growth of U2OS cells were also detected.

[0085] Wherein, the steps of U2OS cell culture include:

[0086] Cells were incubated in DMEM medium supplemented with 10% fetal bovine serum and 100 U / mL penicillin and streptomycin at 37°C, 5% CO 2 conditions, U2OS cells were seeded in 96-well plates (5×10 3 cells / well) and cultured for 12 hours, then added mPG or mPG-TAT with a final concentration of 10 μM for 24 hours or 48 hours after incubation, and set up a DMSO control experimental group at the same time, and then took cell microscope photos or MTT cell viability detection. .

[0087] The experimental steps of MTT cell viability detection include: add 10 μM mPG or mPG-TAT molecules to the cells for 24 hours or 48 hours, add 10 μL MTT solution to each well, so that the final concentration of MTT in each well is 0.5 mg / ml, lightly Mix gently a...

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Abstract

The invention relates to a PDGFR-beta gene expression inhibitor. The inhibitor contains at least one of an mPG molecule and an mPG molecule modified with a cell delivery carrier. The PDGFR-beta gene expression inhibitor contains at least one of mPG molecules and mPG molecules modified with a cell delivery carrier, delivery of the mPG molecules in cells is achieved, PDGFR-beta notch G-quadruplex can be specifically recognized and stabilized in the cells through the mPG molecules, and therefore gene expression of the PDGFR-beta gene expression inhibitor can be regulated in the cells. The expression level of the gene is inhibited.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a PDGFR-β gene expression inhibitor and its application. Background technique [0002] Platelet-derived growth factor (PDGF) is a ubiquitous growth factor encoded by the sis proto-oncogene, which is mainly synthesized by megakaryocytes and plays an important role in tissue damage repair, angiogenesis and cell differentiation. important role. PDGF molecule is a glycoprotein dimer, which can be divided into three types: -AA, -BB and -AB. PDGF and its receptor (Platelet-derived growth factor receptor, PDGFR) are highly expressed in a variety of human tumors, such as pancreatic cancer, small cell lung cancer, gastric cancer and breast cancer. [0003] PDGFR is a receptor tyrosine kinase (RTK) located on the cell surface, which can be divided into two subtypes: PDGFR-α and PDGFR-β. Among them, PDGFR-β can be activated by specifically binding to PDGF-BB or -AB. After being activ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/64A61K47/54A61K31/409A61P9/00A61P35/00A61P43/00
CPCA61K47/545A61K47/64A61K31/409A61P9/00A61P43/00A61P35/00
Inventor 郑克威何意得陈娟南
Owner SUN YAT SEN UNIV
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