Selective alkylation and bioactivity of phosphorothioated nucleolin aptamer AS1411

doi:10.5246/jcps.2017.01.002

Journal of Chinese Pharmaceutical Sciences ›› 2017, Vol. 26 ›› Issue (1): 23-30.DOI: 10.5246/jcps.2017.01.002

• Original articles • Previous Articles Next Articles

Selective alkylation and bioactivity of phosphorothioated nucleolin aptamer AS1411

Guangpu Zhang, Jiali Deng, Xiantao Yang, Yuejie Zhu, Zhu Guan, Lihe Zhang, Zhenjun Yang^*

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China

Received:2016-10-26 Revised:2016-11-21 Online:2017-01-22 Published:2016-12-05
Contact: Tel.: +86-010-82802503, E-mail: yangzj@bjmu.edu.cn
Supported by:
The Ministry of Science and Technology of China (Grant No. 2012CB720604), and the National Natural Science Foundation of China (Grant No. 21332010).

Abstract

Abstract:

An operationally simple and efficient method for the synthesis of a wide range of alkylated nucleotides under mild conditions was developed. This improved method furnishes alkylated nucleotides from both single nucleotides and oligonucleotides, and were prepared in high yields of 81% to 91%. Alkyl modified aptamer AS1411s were synthesized using this method and the biological activity screening results demonstrated that alkylation at the 1^st P-S site on yielded stronger target protein binding capacity, greater growth suppression effects against K562 and HL-60 cell lines, and improved serum stability, as compared with AS1411. This modified aptamer may be useful in tumor detection and treatment.

Key words: Phosphorothioated nucleotide, Alkylation, Aptamer, AS1411, Nucleolin

CLC Number:

R916

Supporting:

Guangpu Zhang, Jiali Deng, Xiantao Yang, Yuejie Zhu, Zhu Guan, Lihe Zhang, Zhenjun Yang. Selective alkylation and bioactivity of phosphorothioated nucleolin aptamer AS1411[J]. Journal of Chinese Pharmaceutical Sciences, 2017, 26(1): 23-30.

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Selective alkylation and bioactivity of phosphorothioated nucleolin aptamer AS1411

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