Cell-penetrating peptide-multi-arm polyethylene glycol-drug conjugate having targeting property and application thereof

A technology of drug conjugates and penetrating peptides, applied in the field of biomedicine, can solve problems such as limited connection sites

Pending Publication Date: 2019-10-18
JENKEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the targeting group is only attached to the...

Method used

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  • Cell-penetrating peptide-multi-arm polyethylene glycol-drug conjugate having targeting property and application thereof
  • Cell-penetrating peptide-multi-arm polyethylene glycol-drug conjugate having targeting property and application thereof
  • Cell-penetrating peptide-multi-arm polyethylene glycol-drug conjugate having targeting property and application thereof

Examples

Experimental program
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Effect test

Embodiment 1 4

[0126] The preparation method of embodiment 1 four-arm PEG-LMWP conjugate (MW10000)

[0127]

[0128] Dissolve LMWP in 20mM KH2PO4 buffer solution, dissolve 4arm PEG-1arm NHS-3arm Opss in DMSO, then add dropwise to the buffer solution, react at room temperature for 2 hours, filter, and purify with a heparin column to obtain the product by freeze-drying Or obtained by precipitation;

Embodiment 2 4

[0129] The preparation method of embodiment 2 four-arm PEG-LMWP-MAL conjugates (MW10000)

[0130]

[0131] Dissolve the 4arm PEG-1arm LMWP-3arm OPSS obtained above in dichloromethane, add appropriate amount of TEA and MAL-NH2, react at room temperature for 12 hours, concentrate the reaction solution, purify, freeze-dry or precipitate the product with isopropanol come out;

Embodiment 3 4

[0132] Example 3 Preparation method of four-arm PEG-LMWP-MAL-RGD conjugate (MW10000)

[0133]

[0134] Dissolve the 4arm PEG-1arm LMWP-MAL-3arm OPSS obtained above in dichloromethane, add an appropriate amount of RGD, react at room temperature for 12 hours, concentrate the reaction solution, purify, freeze-dry or use isopropanol to precipitate the product ;

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Abstract

The invention provides a cell-penetrating peptide-multi-arm polyethylene glycol-drug conjugate which is shown in a general formula I, II, III, IV or V . Compared with a direct-chain type PEG (Polyethylene Glycol)-cell-penetrating peptide conjugate, the multi-arm PEG has a plurality of terminal groups; introducing points having a plurality of functional groups can be connected with different activegroups, so that the problems of limitation of the direct-chain type PEG connection sites, small application range and low drug load capacity are avoided. In addition, The cell-penetrating peptide-multi-arm PEG-drug conjugate provided by the invention has the targeting property, and based on concrete treatment demands, cell-penetrating peptides, drug molecules or PEG chain terminals are connectedwith the targeting groups, so that drugs enter into pathogenic cells in a targeting manner, so that an aim of accurate treatment is fulfilled. The invention also provides application of the cell-penetrating peptide-multi-arm polyethylene glycol-drug conjugate having the targeting property to preparation of targeting drugs, particularly application of the cell-penetrating peptide-multi-arm polyethylene glycol-drug conjugate to treatment of macular degeneration of eyes, asthma and pulmonary fibrosis.

Description

technical field [0001] The invention belongs to the field of biomedicine, in particular to a membrane-penetrating peptide-multi-arm polyethylene glycol-drug conjugate, in particular to a targeted membrane-penetrating peptide-multi-arm polyethylene glycol-drug conjugate Compounds and their applications in biomedicine. Background technique [0002] Cellpenetrating peptides (CPPs) are a class of polypeptides that directly pass through the cell membrane and enter the cell in a non-receptor-dependent manner and non-classical endocytosis. Its length generally does not exceed 30 amino acids and is rich in basic amino acids. The amino acid sequence Usually positively charged, scientists have applied it to gene therapy. Penetrating the cell membrane and entering the cell is a prerequisite for many biological macromolecules with targets in the cell to function. applications in therapeutic areas. [0003] As described in the non-patent literature "Research progress of cell-penetrati...

Claims

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Application Information

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IPC IPC(8): A61K47/60A61K47/64A61K31/7105A61P11/06A61P11/00A61P35/00A61P31/12A61P1/16A61P27/02
CPCA61K47/60A61K47/64A61K31/7105A61P11/06A61P11/00A61P35/00A61P31/12A61P1/16A61P27/02A61K47/42A61K39/395A61K47/10A61K48/00A61K2039/505A61K47/6807A61K47/54A61K47/6835
Inventor 林美娜赵宣朱振刚
Owner JENKEM TECH
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