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Cited by 2,289Advanced biosensing and bioanalysis techniquesRNA Interference and Gene DeliveryDNA and Nucleic Acid Chemistry

Aptamers as therapeutics

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Keefe, Anthony D., Pai, Supriya, Ellington, Andrew·2010·Nature Reviews Drug Discovery
DOI 10.1038/nrd3141PMC PMC7097324
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Abstract

Nucleic acid aptamers can be selected from pools of random-sequence oligonucleotides to bind a wide range of biomedically relevant proteins with affinities and specificities that are comparable to antibodies. Aptamers exhibit significant advantages relative to protein therapeutics in terms of size, synthetic accessibility and modification by medicinal chemistry. Despite these properties, aptamers have been slow to reach the marketplace, with only one aptamer-based drug receiving approval so far. A series of aptamers currently in development may change how nucleic acid therapeutics are perceived. It is likely that in the future, aptamers will increasingly find use in concert with other therapeutic molecules and modalities.

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  • SELEX allows natural selection on oligonucleotides by iterative amplification and selection.

    “In fact, it has become possible to perform natural selection on oligonucleotides by iterative amplification and selection processes using a technique called systematic evolution of ligands by exponential enrichment, or SELEX.”

    From Towards open-ended evolution in self-replicating molecular systems (2017) · cites this paper as [42]

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Authors
Keefe, A. D., Pai, S., & Ellington, A.
Affiliations
The University of Texas at Austin (US)
Corresponding author
Ellington, Andrew
ORCID
Venue
Nature Reviews Drug Discovery
Publisher
Springer Science and Business Media LLC
Published
2010-07
Volume
9
Issue
7
Pages
537-550
ISSN
  • 1474-1776 (ISSN-L)
  • 1474-1784
DOI
10.1038/nrd3141
PMC
PMC7097324
OpenAlex
W2066074720
Cited by
2,289
References
170
Citations by year
2026: 126 · 2025: 154 · 2024: 154 · 2023: 153 · 2022: 190 · 2021: 160 · 2020: 146 · 2019: 132 · 2018: 130 · 2017: 184 · 2016: 171 · 2015: 165 · 2014: 149 · 2013: 106 · 2012: 87
FWCI
7.61
Type
journal article
Language
en
Update notices
erratum (2010-08-01)
Open access
Licence
Locations
  • Nature Reviews Drug Discovery (publishedVersion)
  • PubMed Central (publishedVersion)
  • PubMed (publishedVersion)
Funders
  • Welch Foundation (F-1654)
  • National Institutes of Health
  • National Institute of General Medical Sciences (R01GM077040)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Advanced biosensing and bioanalysis techniques
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA Interference and Gene Delivery
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › DNA and Nucleic Acid Chemistry
Keywords
aptamers, nucleic acid therapeutics, aptamer selection, protein binding, aptamer therapeutics, drug development, oligonucleotide therapeutics
MeSH terms
Animals, DNA, Drug Evaluation, Preclinical, Genetic Techniques, Humans, Ligands, Nucleic Acid Conformation, RNA, RNA, Small Interfering, Aptamers, Nucleotide, Drug Discovery

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