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《第十届全国化学生物学学术会议报告摘要集》2017年
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Alkylation of phosphorothioated thrombin binding aptamer improves the selectivity of inhibiting tumor cell proliferation upon anticoagulation

Yang Xiantao  Zhu Yuejie  Wang Chao  Guan Zhu  Zhang Lihe  Zhenjun Yang  
【摘要】:Aptamers are recently extensively researched for therapy and diagnostic,thrombin binding aptamer is a 15nt deoxyribonucleic acid screened by SELEX that specifically binds to thrombin and inhibits bloodsince it is also endowed with excellent antitumor activity,the intrinsic anticoagulation advantage converted to a main potential side effect for its further application in antiproliferativeSite specific alkylation modification was carried out through nucleophilic reaction of phosphorothioated TBA with bromideThe circular dichroism(CD)spectrums of modified TBAs were weakened and their affinity to thrombin were dramatically reduced reflected by the KD value,on the other hand,their inhibition upon A549 cell were maintained.Generally,incorporation of different alkyls apparently disturbed the binding of TBA to thrombin while keeping the antitumor activity unharmed,thus a new modification strategy was established for the development of TBA as a more selective antitumor agent.

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