Preparation and application of lysosome-targeted senescent cell elimination prodrugs

By designing lysosome-targeted prodrug compounds and utilizing the β-galactosidase activation mechanism unique to senescent cells, selective clearance of senescent cells was achieved, solving the problem of insufficient selectivity in existing technologies and improving clearance efficiency and safety.

CN117603286BActive Publication Date: 2026-09-11JIANGNAN UNIV
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Patent Information

Application Number
CN202311528577.5
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2023-11-15
Publication Date
2026-09-11
Estimated Expiration
2043-11-15

AI Technical Summary

Technical Problem

Existing technologies are unable to effectively and selectively remove senescent cells, resulting in significant toxic side effects on normal cells and impacting tissue regeneration and health.

Method used

A class of lysosome-targeting prodrug compounds were designed. These compounds are activated by β-galactosidase (SA-β-gal) overexpressed in senescent cells to release cytotoxic drugs. By introducing basic lysosome-targeting groups, the selective clearance of senescent cells is improved.

Benefits of technology

It significantly improved the selectivity for senescent cells, reduced the toxic side effects on normal cells, and enhanced the clearance effect on senescent cells. The selectivity index of the preferred compound prodrug A was 2.3 to 2.6 times that of the control drug SSK1.

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Abstract

The application discloses preparation and application of a lysosome-targeted senescent cell clearance prodrug, and belongs to the field of medicinal chemistry. The prodrug takes the lysosome of a senescent cell as a target, is activated by senescence-related beta-galactosidase, and can realize specific clearance of the senescent cell. The prodrug has high selectivity to the senescent cell. The beta-galactosidase-responsive and lysosome-targeted prodrug is a compound of formula 1 or a pharmaceutically acceptable salt, a solvate, an enantiomer, a diastereoisomer, a tautomer or a mixture thereof in any ratio, including a racemic mixture.
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