Reversible regulation of aptamer activity with effector-responsive hairpin oligonucleotides

Na Li

Research output: Contribution to journalArticlepeer-review

3 Scopus citations


Aptamers are oligonucleotides that can bind to various nonnucleic acid molecular targets in a high affinity and specificity. As an emerging class of therapeutic agents, aptamers offer an unparalleled advantage over other classes of therapeutic agents: the possibility to rationally regulate the therapeutic activity of aptamers. Most existing strategies for regulating the aptamer activity have a limited specificity and/or reversibility. Herein we report a simple, generic strategy to simultaneously achieve specificity and reversibility by exploiting the spontaneous conformational change of hairpin oligonucleotides upon the specific recognition of nucleic acid effectors. The effector-responsive hairpin oligonucleotide consists of a sensing loop that recognizes a particular nucleic acid effector, an aptamer stem that inhibits a certain therapeutic target, and an antidote stem that is complementary to the aptamer. Upon the introduction/removal of the effector, the hairpin oligonucleotide undergoes a conformational change that activates/deactivates the aptamer's inhibiting activity on the therapeutic target. This new strategy has been demonstrated with an anticoagulant aptamer that binds and inhibits human α-thrombin.

Original languageEnglish (US)
Pages (from-to)77-84
Number of pages8
JournalJournal of Laboratory Automation
Issue number1
StatePublished - Feb 2013
Externally publishedYes


  • Antidotes
  • Aptamers
  • Hairpin oligonucleotides
  • Nucleic acid effectors
  • Reversible anticoagulant

ASJC Scopus subject areas

  • Computer Science Applications
  • Medical Laboratory Technology


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