He Minze, Wang Zhimin, Wu Xiaoqiu, Du Zhen, Cui Cheng, Zhao Zilong, Sun Yang, Zhang Xiao-Bing, He Lei, Tan Weihong
Molecular Science and Biomedicine Laboratory (MBL), State Key Laboratory of Chemo and Biosensing, College of Chemistry and Chemical Engineering, College of Biology, Aptamer Engineering Center of Hunan Province, Hunan University, Changsha, Hunan, 410082, China.
The Key Laboratory of Zhejiang Province for Aptamers and Theranostics, Zhejiang Cancer Hospital, Hangzhou Institute of Medicine (HIM), Chinese Academy of Sciences, Hangzhou, Zhejiang, 310022, China.
Angew Chem Int Ed Engl. 2025 Jun 24;64(26):e202424687. doi: 10.1002/anie.202424687. Epub 2025 Jun 4.
Aptamers, developed through SELEX (systematic evolution of ligands by exponential enrichment), are generally short oligonucleotide molecules with remarkable specificity and binding affinity to diverse biological targets. These molecules have shown promise across such fields as biosensing, molecular diagnostics, and bioimaging. However, while conventional aptamer selection strategies predominantly emphasize binding affinity, they overlook the broader spectrum of potential biological functionalities. This oversight results in aptamers that frequently exhibit limited capacity for direct biological regulation. This inherent limitation in the selection process significantly constrains both the widespread application of aptamers across diverse fields and their therapeutic potential as direct drug candidates. Functional SELEX represents an advancement by refining selection library construction and selection processes to create F-aptamers that integrate precise molecular recognition with specific biological activities. F-aptamers hold transformative potential as therapeutic agents, diagnostic tools, and molecular regulators, marking a significant step forward in biomedical applications. This minireview critically assesses recent developments in F-aptamer SELEX strategies, addressing challenges, and exploring opportunities for future research in this dynamic field.
通过指数富集配体系统进化技术(SELEX)开发的适配体通常是短寡核苷酸分子,对多种生物靶点具有显著的特异性和结合亲和力。这些分子在生物传感、分子诊断和生物成像等领域已展现出应用前景。然而,传统的适配体筛选策略主要侧重于结合亲和力,却忽视了更广泛的潜在生物学功能。这种忽视导致适配体常常表现出直接生物调节能力有限。筛选过程中的这种固有局限性严重限制了适配体在不同领域的广泛应用及其作为直接候选药物的治疗潜力。功能性SELEX通过优化筛选文库构建和筛选过程来创造融合精确分子识别与特定生物活性的F-适配体,代表了一种进步。F-适配体作为治疗剂、诊断工具和分子调节剂具有变革潜力,标志着生物医学应用向前迈出了重要一步。本综述批判性地评估了F-适配体SELEX策略的最新进展,探讨了该动态领域面临的挑战,并探索了未来研究的机会。