Recent progress of aptamer‒drug conjugates in cancer therapy

Jiaxuan He; Qiao Duan; Chunyan Ran; Ting Fu; Yuan Liu; Weihong Tan

doi:10.1016/j.apsb.2023.01.017

Recent progress of aptamer‒drug conjugates in cancer therapy

Acta Pharm Sin B. 2023 Apr;13(4):1358-1370. doi: 10.1016/j.apsb.2023.01.017. Epub 2023 Jan 26.

Authors

Jiaxuan He¹, Qiao Duan^{1

2}, Chunyan Ran¹, Ting Fu^{1

3}, Yuan Liu¹, Weihong Tan^{1

3

2}

Affiliations

¹ The Cancer Hospital of the University of Chinese Academy of Sciences (Zhejiang Cancer Hospital), The Key Laboratory of Zhejiang Province for Aptamers and Theranostics, Hangzhou Institute of Medicine (HIM), Chinese Academy of Sciences, Hangzhou 310022, China.
² Institute of Molecular Medicine (IMM), Renji Hospital, Shanghai Jiao Tong University School of Medicine, and College of Chemistry and Chemical Engineering, Shanghai Jiao Tong University, Shanghai 200240, China.
³ Molecular Science and Biomedicine Laboratory (MBL), State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, College of Biology, Aptamer Engineering Center of Hunan Province, Hunan University, Changsha 410082, China.

Abstract

Aptamers are single-stranded DNA or RNA sequences that can specifically bind with the target protein or molecule via specific secondary structures. Compared to antibody-drug conjugates (ADC), aptamer‒drug conjugate (ApDC) is also an efficient, targeted drug for cancer therapy with a smaller size, higher chemical stability, lower immunogenicity, faster tissue penetration, and facile engineering. Despite all these advantages, several key factors have delayed the clinical translation of ApDC, such as in vivo off-target effects and potential safety issues. In this review, we highlight the most recent progress in the development of ApDC and discuss solutions to the problems noted above.

Keywords: Aptamer; Aptamer‒drug conjugate; Biotherapeutic drug; Cancer therapy; Drug delivery; Nucleic acid drugs; Small-molecule drug; Therapeutic molecules.

Publication types

Review