The DOI matches its Crossref record; 54 of the 54 references it cites were found in a registry or an index.
Discovery and Development of Therapeutic Aptamers
Abstract
Therapeutic aptamers are single-stranded structured oligonucleotides that bind to protein targets with high affinity and specificity and modulate protein function. Aptamers are discovered by iterative rounds of selection for binding to the target protein, partitioning, and amplification of binding clones from a diverse starting library (SELEX). Postselection optimization of clones using chemical modification is directed at improving affinity, potency, and metabolic stability. A key attribute of therapeutic aptamers is the ability to tailor the pharmacokinetic profile by modulating the degree of metabolic stability and modulating renal clearance and rate of distribution by conjugation to various sizes of polyethylene glycol (PEG). In toxicology studies, therapeutic aptamers have been largely devoid of the previously reported oligonucleotide class effects of immune stimulation, complement activation, and anticoagulation; and the principal finding is the histologically visible accumulation of drug-related material in mononuclear phagocytes, a finding generally not considered an adverse effect. Good safety margins between the pharmacologically effective dose and toxicologically established no-adverse-effect levels have been observed consistently. There are presently seven aptamers either on the market or in clinical trials, but there is still much to be demonstrated in terms of chronic systemic use to fully realize the potential of this promising new class of drugs.
Overview
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Citations
Cites
Tuerk, C., & Gold, L. (1990) · Science · doi:10.1126/science.2200121 · Cited by 10,405
In vitro selection of RNA molecules that bind specific ligands
Ellington, A. D., & Szostak, J. W. (1990) · Nature · doi:10.1038/346818a0 · Cited by 9,812
PEGylation, successful approach to drug delivery
Veronese, F. M., & Pasut, G. (2005) · Drug Discovery Today · doi:10.1016/s1359-6446(05)03575-0 · Cited by 2,339
Pegaptanib, a targeted anti-VEGF aptamer for ocular vascular disease
Ng, E. W. M., Shima, D. T., Calias, P., Cunningham, E. T., Guyer, D. R., & Adamis, A. P. (2006) · Nature Reviews Drug Discovery · doi:10.1038/nrd1955 · Cited by 1,588
The Impact of PEGylation on Biological Therapies
Veronese, F. M., & Mero, A. (2008) · BioDrugs · doi:10.2165/00063030-200822050-00004 · Cited by 1,034
Discovery and development of the G-rich oligonucleotide AS1411 as a novel treatment for cancer
Bates, P. J., Laber, D. A., Miller, D. M., Thomas, S. D., & Trent, J. O. (2009) · Experimental and Molecular Pathology · doi:10.1016/j.yexmp.2009.01.004 · Cited by 874
The Nucleolin Targeting Aptamer AS1411 Destabilizes Bcl-2 Messenger RNA in Human Breast Cancer Cells
Soundararajan, S., Chen, W., Spicer, E. K., Courtenay-Luck, N., & Fernandes, D. J. (2008) · Cancer Research · doi:10.1158/0008-5472.can-07-5723 · Cited by 512
Aptamers as therapeutic and diagnostic agents
Brody, E. N., & Gold, L. (2000) · Reviews in Molecular Biotechnology · doi:10.1016/s1389-0352(99)00004-5 · Cited by 494
Discovery and development of anticancer aptamers
Ireson, C. R., & Kelland, L. R. (2006) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-06-0172 · Cited by 481
Lee, J. F., Stovall, G. M., & Ellington, A. D. (2006) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2006.03.015 · Cited by 398
Cited by
RNA-Based Therapeutics: Current Progress and Future Prospects
Burnett, J. C., & Rossi, J. J. (2012) · Chemistry & Biology · doi:10.1016/j.chembiol.2011.12.008 · Cited by 819
Rohloff, J. C., Gelinas, A. D., Jarvis, T. C., Ochsner, U. A., Schneider, D. J., Gold, L., & Janjic, N. (2014) · Molecular Therapy - Nucleic Acids · doi:10.1038/mtna.2014.49 · Cited by 533
Recent advances in luminescent heavy metal complexes for sensing
Ma, D.-L., Ma, V. P.-Y., Chan, D. S.-H., Leung, K.-H., He, H.-Z., & Leung, C.-H. (2012) · Coordination Chemistry Reviews · doi:10.1016/j.ccr.2012.07.005 · Cited by 296
Active targeting of gold nanoparticles as cancer therapeutics
Goddard, Z. R., Marín, M. J., Russell, D. A., & Searcey, M. (2020) · Chemical Society Reviews · doi:10.1039/d0cs01121e · Cited by 282
Nucleic acid aptamers in cancer research, diagnosis and therapy
Ma, H., Liu, J., Ali, M. M., Mahmood, M. A. I., Labanieh, L., Lu, M., Iqbal, S. M., Zhang, Q., Zhao, W., & Wan, Y. (2015) · Chemical Society Reviews · doi:10.1039/c4cs00357h · Cited by 265
Metadata
- Authors
- Bouchard, P. R., Hutabarat, R. M., & Thompson, K. M.
- Venue
- Annual Review of Pharmacology and Toxicology
- Publisher
- Annual Reviews
- Published
- 2010-02-01
- Volume
- 50
- Issue
- 1
- Pages
- 237-257
- ISSN
- 0362-1642 (ISSN-L)
- 1545-4304
- OpenAlex
- W2116641087
- Cited by
- 320
- References
- 54
- FWCI
- 1.83
- Type
- journal article
- Language
- en
- Open access
- closed
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
How to cite
Cite CoChat for the checks on this page, and the paper for its own findings.
- This page
- CoChat. (2026). Citation check: Discovery and Development of Therapeutic Aptamers. https://app.cochat.ai/papers/10.1146/annurev.pharmtox.010909.105547
- The paper
- Bouchard, P. R., Hutabarat, R. M., & Thompson, K. M. (2010). Discovery and Development of Therapeutic Aptamers. Annual Review of Pharmacology and Toxicology. https://doi.org/10.1146/annurev.pharmtox.010909.105547
Data sources
Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
