Aptamers: Uptake mechanisms and intracellular applications

Adv Drug Deliv Rev. 2018 Sep:134:22-35. doi: 10.1016/j.addr.2018.07.003. Epub 2018 Jul 6.

Abstract

The structural flexibility and small size of aptamers enable precise recognition of cellular elements for imaging and therapeutic applications. The process by which aptamers are taken into cells depends on their targets but is typically clathrin-mediated endocytosis or macropinocytosis. After internalization, most aptamers are transported to endosomes, lysosomes, endoplasmic reticulum, Golgi apparatus, and occasionally mitochondria and autophagosomes. Intracellular aptamers, or "intramers," have versatile functions ranging from intracellular RNA imaging, gene regulation, and therapeutics to allosteric modulation, which we discuss in this review. Immune responses to therapeutic aptamers and the effects of G-quadruplex structure on aptamer function are also discussed.

Keywords: Allosteric modulation; Aptamer; Endocytosis; G-quadruplex; Gene regulation; Imaging; Intramers.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Aptamers, Nucleotide / chemistry
  • Aptamers, Nucleotide / metabolism*
  • Aptamers, Nucleotide / pharmacokinetics*
  • Aptamers, Nucleotide / pharmacology
  • Drug Evaluation, Preclinical
  • Fluorescence Resonance Energy Transfer
  • Humans
  • Optical Imaging
  • Transcription Factors / antagonists & inhibitors
  • Transcription Factors / metabolism

Substances

  • Aptamers, Nucleotide
  • Transcription Factors