ArticleNucleic acids research2015
Site specific replacements of a single loop nucleoside with a dibenzyl linker may switch the activity of TBA from anticoagulant to antiproliferative.
Article in Nucleic acids research, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 46 citations in OpenAlex.
- Probing the Effects of Chemical Modifications on Anticoagulant and Antiproliferative Activity of Thrombin Binding Aptamer.International journal of molecular sciences · 2024Article
- Unlocking precision in aptamer engineering: a case study of the thrombin binding aptamer illustrates why modification size, quantity, and position matter.Nucleic acids research · 2024Article
- Aptamer AS411 interacts with the KRAS promoter/hnRNP A1 complex and shows increased potency against drug-resistant lung cancer.RSC medicinal chemistry · 2024Article
- Improving the Biological Properties of Thrombin-Binding Aptamer by Incorporation of 8-Bromo-2'-Deoxyguanosine and 2'-Substituted RNA Analogues.International journal of molecular sciences · 2023Article
- Steric hindrance and structural flexibility shape the functional properties of a guanine-rich oligonucleotide.Nucleic acids research · 2023Article
- Properties and Potential Antiproliferative Activity of Thrombin-Binding Aptamer (TBA) Derivatives with One or Two Additional G-Tetrads.International journal of molecular sciences · 2022Article
- Structure- and Interaction-Based Design of Anti-SARS-CoV-2 Aptamers.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- A Comprehensive Analysis of the Thrombin Binding Aptamer Containing Functionalized Pyrrolo-2'-deoxycytidines.Pharmaceuticals (Basel, Switzerland) · 2021Article
- G-Quadruplex-Based Drug Delivery Systems for Cancer Therapy.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Exploring New Potential Anticancer Activities of the G-Quadruplexes Formed by [(GTGInternational journal of molecular sciences · 2021Article
- Structural properties and anticoagulant/cytotoxic activities of heterochiral enantiomeric thrombin binding aptamer (TBA) derivatives.Nucleic acids research · 2020Article
- Evolution of a highly functional circular DNA aptamer in serum.Nucleic acids research · 2020Article
- Spectroscopic Properties of Two 5'-(4-Dimethylamino)Azobenzene Conjugated G-Quadruplex Forming Oligonucleotides.International journal of molecular sciences · 2020Article
- uL3 Mediated Nucleolar Stress Pathway as a New Mechanism of Action of Antiproliferative G-quadruplex TBA Derivatives in Colon Cancer Cells.Biomolecules · 2020Article
- G-Quadruplex-Forming Aptamers-Characteristics, Applications, and Perspectives.Molecules (Basel, Switzerland) · 2019Review
- Bimodular Antiparallel G-Quadruplex Nanoconstruct with Antiproliferative Activity.Molecules (Basel, Switzerland) · 2019Article
- Investigating the properties of TBA variants with twin thrombin binding domains.Scientific reports · 2019Article
- Crystal structures of thrombin in complex with chemically modified thrombin DNA aptamers reveal the origins of enhanced affinity.Nucleic acids research · 2018Article
- Thermodynamic, Anticoagulant, and Antiproliferative Properties of Thrombin Binding Aptamer Containing Novel UNA Derivative.Molecular therapy. Nucleic acids · 2018Article
- Studying DNA G-Quadruplex Aptamer byACS omega · 2017Article
Corrections and comments
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Authors and funding
13 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Many antiproliferative G-quadruplexes (G4s) arise from the folding of GT-rich strands. Among these, the Thrombin Binding Aptamer (TBA), as a rare example, adopts a monomolecular well-defined G4 structure. Nevertheless, the potential anticancer properties of TBA are severely hampered by its anticoagulant action and, consequently, no related studies have appeared so far in the literature. We wish to report here that suitable chemical modifications in the TBA sequence can preserve its antiproliferative over anticoagulant activity. Particularly, we replaced one residue of the TT or TGT loops with a dibenzyl linker to develop seven new quadruplex-forming TBA based sequences (TBA-bs), which were studied for their structural (CD, CD melting, 1D NMR) and biological (fibrinogen, PT and MTT assays) properties. The three-dimensional structures of the TBA-bs modified at T13 (TBA-bs13) or T12 (TBA-bs12), the former endowed with selective antiproliferative activity, and the latter acting as potently as TBA in both coagulation and MTT assays, were further studied by 2D NMR restrained molecular mechanics. The comparative structural analyses indicated that neither the stability, nor the topology of the G4s, but the different localization of the two benzene rings of the linker was responsible for the loss of the antithrombin activity for TBA-bs13.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.