ArticleChemical biology & drug design2011
A disalicylic acid-furanyl derivative inhibits ephrin binding to a subset of Eph receptors.
Article in Chemical biology & drug design, 2011. 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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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
25 citing papers in PubMed, 40 citations in OpenAlex.
- Exploring the potential of EphA2 receptor signaling pathway: a comprehensive review in cancer treatment.Molecular biology reports · 2024Review
- Lipidation and PEGylation Strategies to Prolong theEuropean journal of medicinal chemistry · 2023Article
- Targeting EPHA2 with Kinase Inhibitors in Colorectal Cancer.ChemMedChem · 2023Article
- Eph Receptors in Cancer.Biomedicines · 2023Review
- NMR-Guided Design of Potent and Selective EphA4 Agonistic Ligands.Journal of medicinal chemistry · 2021Article
- Targeting EphA2 in cancer.Journal of hematology & oncology · 2020Review
- Therapeutic potential of targeting the Eph/ephrin signaling complex.The international journal of biochemistry & cell biology · 2018Review
- Author Correction: Ephrin receptor A2 is an epithelial cell receptor for Epstein-Barr virus entry.Nature microbiology · 2018Article
- Author Correction: EphA2 is an epithelial cell pattern recognition receptor for fungal β-glucans.Nature microbiology · 2018Article
- The Role of Ephs and Ephrins in Memory Formation.The international journal of neuropsychopharmacology · 2016Review
- Eph receptor tyrosine kinases in cancer stem cells.Cytokine & growth factor reviews · 2015Review
- UniPR129 is a competitive small molecule Eph-ephrin antagonist blocking in vitro angiogenesis at low micromolar concentrations.British journal of pharmacology · 2014Article
- On the use of 2,5-dimethyl-pyrrol-1-yl-benzoic acid derivatives as EPH-ephrin antagonists.Journal of virology · 2014Article
- Blockade of EphA4 signaling ameliorates hippocampal synaptic dysfunctions in mouse models of Alzheimer's disease.Proceedings of the National Academy of Sciences of the United States of America · 2014Article
- Therapeutic targeting of EPH receptors and their ligands.Nature reviews. Drug discovery · 2014Review
- Synthesis and structure-activity relationships of amino acid conjugates of cholanic acid as antagonists of the EphA2 receptor.Molecules (Basel, Switzerland) · 2013Article
- Amino acid conjugates of lithocholic acid as antagonists of the EphA2 receptor.Journal of medicinal chemistry · 2013Article
- HTS by NMR of combinatorial libraries: a fragment-based approach to ligand discovery.Chemistry & biology · 2013Article
- Article
- Eph receptors and ephrins as targets for cancer therapy.Journal of cellular and molecular medicine · 2012Review
Corrections and comments
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Authors and funding
12 authors at 2 institutions in 2 countries.
Funding
Abstract
Eph receptor tyrosine kinases and ephrin ligands control many physiological and pathological processes, and molecules interfering with their interaction are useful probes to elucidate their complex biological functions. Moreover, targeting Eph receptors might enable new strategies to inhibit cancer progression and pathological angiogenesis as well as promote nerve regeneration. Because our previous work suggested the importance of the salicylic acid group in antagonistic small molecules targeting Eph receptors, we screened a series of salicylic acid derivatives to identify novel Eph receptor antagonists. This identified a disalicylic acid-furanyl derivative that inhibits ephrin-A5 binding to EphA4 with an IC(50) of 3 μm in ELISAs. This compound, which appears to bind to the ephrin-binding pocket of EphA4, also targets several other Eph receptors. Furthermore, it inhibits EphA2 and EphA4 tyrosine phosphorylation in cells stimulated with ephrin while not affecting phosphorylation of EphB2, which is not a target receptor. In endothelial cells, the disalicylic acid-furanyl derivative inhibits EphA2 phosphorylation in response to TNFα and capillary-like tube formation on Matrigel, two effects that depend on EphA2 interaction with endogenous ephrin-A1. These findings suggest that salicylic acid derivatives could be used as starting points to design new small molecule antagonists of Eph receptors.
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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.