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Nucleic acid aptamer-paclitaxel coupling with combined targeted drug is a novel strategy that uses nucleic acid aptamer as a targeted molecule to couple paclitaxel as an anticancer drug, so as to achieve accurate diagnosis and treatment of tumor cells. Aptamers are a nucleic acid molecule with high affinity and high specificity obtained through systematic evolutionary screening, which can bind to a variety of targets, such as proteins, cells, tissues, etc. Paclitaxel, a natural product derived from taxane bark, suppresses microtubule polymerization and blocks cell division, and is a widely used chemotherapeutic agent for the treatment of various cancers. Nucleic acid aptamer-paclitaxel coupling can use the targeting of nucleic acid aptamer to effectively deliver paclitaxel to the tumor site, thus improving the therapeutic efficacy and safety of drugs.

A coupling compound based on the nucleic acid aptamer AS1411 and paclitaxel that inhibits the growth and survival of multiple myeloma (MM) cells. This coupling can specifically bind to the nucleolar component C (NCL) on the surface of MM cells, and enter cells by endocytosis, release paclitaxel and thereby induce apoptosis. This coupling inhibited growth in a mouse MM tumor model without significant toxic side effects.

A coupling compound based on the nucleic acid aptamer Apt 22 and paclitaxel that targets mucin 1 (MUC 1) on the surface of lung cancer cells. This coupling compound efficiently binds to MUC 1-positive lung cancer cells and enters the cells by endocytosis, releasing paclitaxel, thereby inhibiting cell proliferation and migration. It was also demonstrated that the coupling can prolong the survival of a mouse lung cancer model with lower toxicity.