Inhibition of thrombin activity by a covalent-binding aptamer and reversal by the complementary strand antidote

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Abstract

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.

source:https://doi.org/10.1039/D0CC08109D

Journal

  • Chemical Communications

    Chemical Communications 57 (20), 2483-2486, 2021-03-11

    The Royal Society of Chemistry (RSC)

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