ArticleThe Biochemical journal2014
Identification and characterization of a mirror-image oligonucleotide that binds and neutralizes sphingosine 1-phosphate, a central mediator of angiogenesis.
Article in The Biochemical journal, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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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.
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Who cites it
13 citing papers in PubMed, 22 citations in OpenAlex.
- Spiegelmer Aptamers: Innovative Approach in Breast Cancer.Breast cancer : basic and clinical research · 2026Review
- Emerging role of nucleic acid aptamers in sepsis-induced coagulopathy: Future perspectives in diagnostics and therapeutics.Annals of intensive care · 2026Review
- Advances in TherapeuticGenes · 2021Review
- Modified Nucleic Acids: Expanding the Capabilities of Functional Oligonucleotides.Molecules (Basel, Switzerland) · 2020Review
- Long noncoding RNAs: emerging roles in pulmonary hypertension.Heart failure reviews · 2020Review
- Predicting Future Prospects of Aptamers in Field-Effect Transistor Biosensors.Molecules (Basel, Switzerland) · 2020Article
- Aptamer-field-effect transistors overcome Debye length limitations for small-molecule sensing.Science (New York, N.Y.) · 2018Article
- Sphingosine 1-phosphate signaling impacts lymphocyte migration, inflammation and infection.Pathogens and disease · 2016Review
- Sphingosine-1 Phosphate: A New Modulator of Immune Plasticity in the Tumor Microenvironment.Frontiers in oncology · 2016Review
- Selection and Biosensor Application of Aptamers for Small Molecules.Frontiers in chemistry · 2016Review
- Generation of Aptamers with an Expanded Chemical Repertoire.Molecules (Basel, Switzerland) · 2015Review
- A novel CGRP-neutralizing Spiegelmer attenuates neurogenic plasma protein extravasation.British journal of pharmacology · 2015Article
- Stereospecificity of oligonucleotide interactions revisited: no evidence for heterochiral hybridization and ribozyme/DNAzyme activity.PloS one · 2015Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The sphingolipid S1P (sphingosine 1-phosphate) is known to be involved in a number of pathophysiological conditions such as cancer, autoimmune diseases and fibrosis. It acts extracellularly through a set of five G-protein-coupled receptors, but its intracellular actions are also well documented. Employing in vitro selection techniques, we identified an L-aptamer (Spiegelmer®) to S1P designated NOX-S93. The binding affinity of NOX-S93 to S1P had a Kd value of 4.3 nM. The Spiegelmer® shows equal binding to dihydro-S1P, but no cross-reactivity to the related lipids sphingosine, lysophosphatidic acid, ceramide, ceramide-1-phosphate or sphingosine phosphocholine. In stably transfected CHO (Chinese-hamster ovary) cell lines expressing the S1P receptors S1PR1 or S1PR3, NOX-S93 inhibits S1P-mediated β-arrestin recruitment and intracellular calcium release respectively, with IC50 values in the low nanomolar range. The pro-angiogenic activity of S1P, and of the growth factors VEGF-A (vascular endothelial growth factor-A), FGF-2 (fibroblast growth factor-2) and IGF-1 (insulin-like growth factor-1), was effectively blocked by NOX-S93 in a cellular angiogenesis assay employing primary human endothelial cells. These data provide further evidence for the relevance of extracellular S1P as a central mediator of angiogenesis, suggesting pharmacological S1P neutralization as a promising treatment alternative to current anti-angiogenesis approaches.
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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 OpenQuestion graph.