Polypeptide probe for cancer treatment and preparation method and application thereof
A probe and fluorescent probe technology, applied in the field of polypeptide probes and their preparation, can solve the problems of the influence of organelle destruction not yet fully elucidated, the long escape time of nano-drugs, etc., and achieve strong targeting ability and high delivery efficiency. Effect
Pending Publication Date: 2022-05-31
山东雷泽生物科技有限责任公司
View PDF0 Cites 0 Cited by
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Although the above modification methods can promote the escape of nanomedicines from lysosomes, the escape time of nanomedicines from lysosomes in the above methods is long, and the impact of nanomedicines on organelle damage when they escape from lysosomes has not been fully elucidated.
More importantly, nanomedicine still needs to enter the lysosome and then escape from the lysosome, so it cannot exert its therapeutic effect at its maximum effect
Method used
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View moreImage
Smart Image Click on the blue labels to locate them in the text.
Smart ImageViewing Examples
Examples
Experimental program
Comparison scheme
Effect test
Embodiment 1
[0066] 1. Synthesis of peptide probes (such as figure 2 ):
[0067] In a 10 mL round bottom flask, add Pal (PalGGGHGPLGLAGGGKGGGPAPra-NH 2 ) (29.3 mg, 15 μmol), klaklakklaklakCGKRK-NH 2 (20.9 mg, 10 μmol), tris(2-carboxyethyl) phosphine (1.4 mg, 5 μmol), 2 mL of dimethyl sulfoxide, 2 mL of phosphate buffered saline solution, under the protection of nitrogen atmosphere, the reaction was stirred at room temperature for 24 h to obtain the crude product , purified by high performance liquid chromatography at a speed of 2mL / min, solvent B was eluted with gradient from 20% to 100% for 50 minutes, wherein solvent A was water (containing 0.1% trifluoroacetic acid solution), solvent B was acetonitrile (containing 0.1% trifluoroacetic acid solution) 0.1% trifluoroacetic acid solution). After purification, it was freeze-dried to obtain the intermediate product polypeptide PK (20.5 mg, yield: 51%).
[0068] PyTPA (6.8mg, 10μmol), intermediate product polypeptide PK (20.3mg, 5μmol), c...
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More PUM
Login to View More Abstract
The invention provides a polypeptide probe for cancer treatment and a preparation method and application thereof. The polypeptide probe PKP is composed of a polypeptide Pal and a polypeptide KP part. The polypeptide probe PKP can be divided into two parts under the stimulation of matrix metalloproteinase 2 which is highly expressed in a tumor microenvironment, the Pal part rapidly enters cancer cells and forms nanofibers in lysosomes, so that protein phosphatase 2A is reduced, and meanwhile, the KP part slowly enters the cancer cells, so that the protein phosphatase 2A is reduced. And the endocytosis pathway is converted from gridding protein-mediated endocytosis to cell cellar-mediated endocytosis, so that the cells are prevented from being trapped in lysosome and reaching mitochondria, cancer cells are killed through photodynamic therapy, and the effect of cancer treatment is achieved. According to the invention, the polypeptide-based probe is used for cancer treatment for the first time to self-regulate the endocytosis pathway, so that the probe is prevented from being trapped in lysosome and the effect of the probe is exerted to the maximum extent.
Description
technical field [0001] The invention relates to the application technology of molecular probes and the field of cancer treatment, in particular to a polypeptide probe for inhibiting, delaying and reducing the growth of cancer and a preparation method and application thereof. Background technique [0002] Today, nanomedicine is an emerging product generated by the combination of nanotechnology and medicine, as one of the new drugs for diagnosis, treatment and prevention of tumor and immune diseases. Due to the aggregation of nanomedicines at tumor and inflammatory sites after intravenous injection, researchers are promoting them to the field of tumor therapy. Nanomedicines based on nanotechnology have the characteristics of diversity, targeting, sustained release, tumor site aggregation and good biocompatibility, so they have higher therapeutic efficiency than traditional medicines. However, when nanodrugs successfully cross the barrier of targeting tumor cells, there remain...
Claims
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More Application Information
Patent Timeline
Login to View More IPC IPC(8): C07K14/00C07K1/16A61K41/00A61K47/64A61K49/00A61P35/00
CPCC07K14/00A61K41/0057A61K47/64A61K49/0021A61K49/0056A61P35/00
Inventor 娄筱叮夏帆杨聚梁胡晶晶魏佳明
Owner 山东雷泽生物科技有限责任公司