Dual-target nucleic acid aptamers, conjugates, preparation methods and applications

By constructing a stable conjugation between Nectin4 and c-Met dual-target nucleic acid aptamers and MMAE, the problem of insufficient tumor selectivity of MMAE in vivo was solved, achieving highly efficient targeted therapy and drug delivery for bladder cancer, and enhancing anti-tumor activity and safety.

CN122303245APending Publication Date: 2026-06-30HANGZHOU INSTITUTE OF MEDICAL SCIENCES CHINESE ACADEMY OF SCIENCES

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
HANGZHOU INSTITUTE OF MEDICAL SCIENCES CHINESE ACADEMY OF SCIENCES
Filing Date
2026-05-21
Publication Date
2026-06-30

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Abstract

This invention provides a dual-target nucleic acid aptamer, conjugate, preparation method, and application. Using Nectin4 and c-Met as dual targets, this invention designs and constructs a dual-target nucleic acid aptamer-MMAE conjugate. Stable conjugation between the nucleic acid aptamer and MMAE is achieved through a maleimide-thiol specific reaction. Through systematic structural characterization, in vitro functional verification, and in vivo imaging and therapeutic studies, the invention verifies the conjugate's targeting ability for bladder cancer, in vitro antitumor activity, and in vivo tumor enrichment and growth inhibition effects. This addresses the problem of insufficient MMAE targeting, providing a new experimental model and theoretical basis for nucleic acid aptamer-mediated targeted delivery of small molecule cytotoxic drugs, and exploring new strategies for dual-target precision treatment of bladder cancer.
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