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

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...

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Problems solved by technology

However, the targeting group is only attached to the penetrating peptide, and the attachment sites are limited

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