- Photosensitizer-peptide conjugates with cleavable linkers and a composition for photodynamic diagnosis and therapy comprising the same

摘要

The present invention relates to a conjugate for photodynamic diagnosis or treatment in which a peptide is bound to a photosensitizer through a linkage capable of intracellular degradation, and a composition for photodynamic diagnosis or treatment comprising the conjugate. In the photosensitizer-peptide conjugate of the present invention, when the distance between the photosensitizer and the tryptophan is 2 nm or less through the decomposable linkage, the fluorescence signal of the photosensitizer and the reactive oxygen generating ability are quenched, It does not generate fluorescence signals in the tissues or during the circulation of blood, nor does it produce reactive oxygen. When the binding of the present invention is selectively taken into cells by interaction with an overexpressed antigen on the surface of a target cell, the distance between the tryptophan contained in the peptide and the photosensitizer contained in the peptide is 2 nm As far as it goes away and the extinction action disappears, strong fluorescence signal generation and reactive oxygen production are actively occurring. Accordingly, the photodynamic diagnostic or therapeutic conjugate comprising the peptide according to the present invention has high tissue permeability and is safe in normal cells, but exhibits a high photodynamic therapeutic effect only in target cells (for example, cancer cells), and has a high target signal ratio A good diagnostic image can be obtained.