ArticleInternational journal of molecular sciences2020
Design, Synthesis and Characterization of Cyclic NU172 Analogues: A Biophysical and Biological Insight.
Article in International journal of molecular sciences, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
17 citing papers in PubMed, 34 citations in OpenAlex.
- Folding and unfolding dynamics of a DNA aptamer studied by heteronuclearJournal of magnetic resonance (San Diego, Calif. : 1997) · 2026Article
- Recent Advances in Aptamer-Based Applications in Cardiology.International journal of molecular sciences · 2026Review
- Large-scale multi-omic biosequence transformers for modeling protein-nucleic acid interactions.PloS one · 2026Article
- Large-Scale Multi-omic Biosequence Transformers for Modeling Protein-Nucleic Acid Interactions.ArXiv · 2025Article
- Probing the Effects of Chemical Modifications on Anticoagulant and Antiproliferative Activity of Thrombin Binding Aptamer.International journal of molecular sciences · 2024Article
- A Survey on Computational Methods in Drug Discovery for Neurodegenerative Diseases.Biomolecules · 2024Review
- A bimolecular modification strategy for developing long-lasting bone anabolic aptamer.Molecular therapy. Nucleic acids · 2023Article
- Applications and future of aptamers that achieve rapid-onset anticoagulation.RNA (New York, N.Y.) · 2023Article
- A terminal functionalization strategy reveals unusual binding abilities of anti-thrombin anticoagulant aptamers.Molecular therapy. Nucleic acids · 2022Article
- Aptamers Regulating the Hemostasis System.Molecules (Basel, Switzerland) · 2022Review
- Truncated Analogues of a G-Quadruplex-Forming Aptamer Targeting Mutant Huntingtin: Shorter Is Better!International journal of molecular sciences · 2022Article
- Fighting the Huntington's Disease with a G-Quadruplex-Forming Aptamer Specifically Binding to Mutant Huntingtin Protein: Biophysical Characterization, In Vitro and In Vivo Studies.International journal of molecular sciences · 2022Article
- Aptamers: Functional-Structural Studies and Biomedical Applications.International journal of molecular sciences · 2022Article
- Controlling Coagulation in Blood with Red Light.Angewandte Chemie (International ed. in English) · 2021Article
- Beyond G-Quadruplexes-The Effect of Junction with Additional Structural Motifs on Aptamers Properties.International journal of molecular sciences · 2021Review
- Charge-Transfer Interactions Stabilize G-Quadruplex-Forming Thrombin Binding Aptamers and Can Improve Their Anticoagulant Activity.International journal of molecular sciences · 2021Article
- Dimeric and Multimeric DNA Aptamers for Highly Effective Protein Recognition.Molecules (Basel, Switzerland) · 2020Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
NU172-a 26-mer oligonucleotide able to bind exosite I of human thrombin and inhibit its activity-was the first aptamer to reach Phase II clinical studies as an anticoagulant in heart disease treatments. With the aim of favoring its functional duplex-quadruplex conformation and thus improving its enzymatic stability, as well as its thrombin inhibitory activity, herein a focused set of cyclic NU172 analogues-obtained by connecting its 5'- and 3'-extremities with flexible linkers-was synthesized. Two different chemical approaches were exploited in the cyclization procedure, one based on the oxime ligation method and the other on Cu(I)-assisted azide-alkyne cycloaddition (CuAAC), affording NU172 analogues including circularizing linkers with different length and chemical nature. The resulting cyclic NU172 derivatives were characterized using several biophysical techniques (ultraviolet (UV) and circular dichroism (CD) spectroscopies, gel electrophoresis) and then investigated for their serum resistance and anticoagulant activity in vitro. All the cyclic NU172 analogues showed higher thermal stability and nuclease resistance compared to unmodified NU172. These favorable properties were, however, associated with reduced-even though still significant-anticoagulant activity, suggesting that the conformational constraints introduced upon cyclization were somehow detrimental for protein recognition. These results provide useful information for the design of improved analogues of NU172 and related duplex-quadruplex structures.
Indexed as
Identifiers
What Socratic holds
Registered trials
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 Socratic graph.