Synthesis of a Terminal Amino‐Modified Nucleolin Aptamer and Its Paclitaxel Conjugate. Issue 35 (15th September 2022)

• Record Type: Journal Article
• Authors: Xu, Xiaoling; Jiang, Mingyu; Miao, Dan; Liu, Yongping; Tan, Xiaobin; Hu, Jiawei; Gu, Chunye; Peng, Weijie; Jiang, Feng
• Is Part Of: ChemistrySelect. Volume 7:Issue 35(2022)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2022-09-15
• Subjects: Aptamer-drug conjugate -- Amino space modified CPG -- Terminal amino-modification nucleolin aptamer -- Paclitaxel conjugate -- Target delivery; Chemistry -- Periodicals; 540.5
• DOI: 10.1002/slct.202202781
• Languages: English
• ISSNs: 2365-6549

Abstract

Abstract: Aptamer‐drug conjugate has been developed as a potential class of targeted therapeutics, which using aptamer as tumor recognition elements could targeted deliver the conjugated chemically toxic drug to tumor site. One of the keys to the success of aptamer‐drug conjugate is terminal modification of aptamer to facilitate the conjugation with drugs. Herein, a novel terminal amino‐modified nucleolin aptamer which using solketal as raw material was developed. Moreover, its paclitaxel conjugate wherein the aptamer coupled with paclitaxel derivatives by amidation was also conducted. The easily available raw materials, stable structure, together with its simplicity of operation, gives it the potential for use on an industrial scale. Abstract : Aptamer‐drug conjugate has been developed as a potential class of targeted therapeutics, which using aptamer as tumor recognition elements could targeted deliver the conjugated chemically toxic drug to tumor site. One of the keys to the success of aptamer‐drug conjugate is terminal modification of aptamer to facilitate the conjugation with drugs. Herein, a novel terminal amino‐modified nucleolin aptamer which using solketal as raw material was developed. Moreover, its paclitaxel conjugate wherein the aptamer coupled with paclitaxel derivatives by amidation was also conducted. The easily available raw materials, stable structure, together with its simplicity of operation, gives it the potential for use on an industrial scale.