期刊
CHEMICAL COMMUNICATIONS
卷 57, 期 20, 页码 2483-2486出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/d0cc08109d
关键词
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资金
- JSPS KAKENHI grant [20J22890]
- Grants-in-Aid for Scientific Research [20J22890] Funding Source: KAKEN
This study created a DNA-aptamer-type covalent drug which can be deactivated and reactivated through a specific structure, providing a new approach to alleviate irreversible adverse drug effects.
Alleviating the potential risk of irreversible adverse drug effects has been an important and challenging issue for the development of covalent drugs. Here we created a DNA-aptamer-type covalent drug by introducing a sulfonyl fluoride warhead at appropriate positions of the thrombin binding aptamer to create weaponized covalent drugs. We showed the de-activation of thrombin by the novel modality, followed by its re-activation by the complementary strand antidote at an arbitrary time. We envision that such on-demand reversal of covalent drugs will alleviate the major concern of potentially irreversible ADEs and accelerate the translational application of covalent aptamer drugs.
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