Cited by 305Advanced biosensing and bioanalysis techniquesRNA Interference and Gene DeliveryDNA and Nucleic Acid Chemistry

The DOI matches its Crossref record; 115 of the 115 references it cites were found in a registry or an index.

Aptamers: A Review of Their Chemical Properties and Modifications for Therapeutic Application

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Abstract

Aptamers are short, single-stranded oligonucleotides that bind to specific target molecules. The shape-forming feature of single-stranded oligonucleotides provides high affinity and excellent specificity toward targets. Hence, aptamers can be used as analogs of antibodies. In December 2004, the US Food and Drug Administration approved the first aptamer-based therapeutic, pegaptanib (Macugen), targeting vascular endothelial growth factor, for the treatment of age-related macular degeneration. Since then, however, no aptamer medication for public health has appeared. During these relatively silent years, many trials and improvements of aptamer therapeutics have been performed, opening multiple novel directions for the therapeutic application of aptamers. This review summarizes the basic characteristics of aptamers and the chemical modifications available for aptamer therapeutics.

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Crossref · 10.3390/molecules24234229

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Figures

Figure 1 Overall structure of known aptamer–protein complexes with electrostatic surface potential [5]. The RNA aptamer is represented by a yellow ball-and-stick model. (A) Aptamer–thrombin complex at 1.8 Å resolution [13]. (B) Aptamer–nuclear factor-κB complex at 2.45 Å resolution [11]. (C) Aptamer–MS2 coat protein complex at 2.8 Å resolution [12]. (D) Aptamer–Fc region of human IgG1 (hFc1) complex at 2.15 Å resolution [16]. Blue areas: positively charged; red areas: negatively charged.
Figure 1 Overall structure of known aptamer–protein complexes with electrostatic surface potential [5]. The RNA aptamer is represented by a yellow ball-and-stick model. (A) Aptamer–thrombin complex at 1.8 Å resolution [13]. (B) Aptamer–nuclear factor-κB complex at 2.45 Å resolution [11]. (C) Aptamer–MS2 coat protein complex at 2.8 Å resolution [12]. (D) Aptamer–Fc region of human IgG1 (hFc1) complex at 2.15 Å resolution [16]. Blue areas: positively charged; red areas: negatively charged.CC BY · PubMed Central
Figure 2 Chemical structure of a polynucleotide element. Modifications at the indicated positions are shown. OMe: O-methylation, LNA: locked nucleic acid, PEG: polyethylene glycol.
Figure 2 Chemical structure of a polynucleotide element. Modifications at the indicated positions are shown. OMe: O-methylation, LNA: locked nucleic acid, PEG: polyethylene glycol.CC BY · PubMed Central

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Metadata

Authors
Adachi, T., & Nakamura, Y.
Affiliations
  • RIBOMIC Inc., Minato-ku, Tokyo 108-0071, Japan
  • Institute of Medical Science, The University of Tokyo (JP)
Corresponding author
Adachi, Tatsuo
Venue
Molecules
Publisher
MDPI AG
Published
2019-11-21
Volume
24
Issue
23
Pages
4229
ISSN
1420-3049 (ISSN-L)
OpenAlex
W2989998401
Cited by
300
References
115
Citations by year
2026: 33 · 2025: 50 · 2024: 59 · 2023: 53 · 2022: 44 · 2021: 42 · 2020: 19
FWCI
2.32
Type
journal article
Language
en
Open access
Locations
  • Molecules (publishedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
Funders
University of Tokyo
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, aptamer therapeutics, chemical modification, oligonucleotide chemistry, pegaptanib, vascular endothelial growth factor, age-related macular degeneration, drug delivery
MeSH terms
Animals, Humans, Infections, Neoplasms, Aptamers, Nucleotide, Drug Discovery

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