ArticleJournal of medicinal chemistry2011
Design, synthesis, and structure-activity relationship exploration of 1-substituted 4-aroyl-3-hydroxy-5-phenyl-1H-pyrrol-2(5H)-one analogues as inhibitors of the annexin A2-S100A10 protein interaction.
Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 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
21 citing papers in PubMed, 65 citations in OpenAlex.
- Influence of substitution patterns on the antimicrobial properties of pyrrole sulfonamide scaffolds.Frontiers in chemistry · 2026Article
- Article
- Synthetic Approaches to Novel Human Carbonic Anhydrase Isoform Inhibitors Based on Pyrrol-2-one Moiety.Journal of medicinal chemistry · 2024Article
- S100A10 promotes cancer metastasis via recruitment of MDSCs within the lungs.Oncoimmunology · 2024Article
- Stereoselective, Multicomponent Approach to Quaternary Substituted Hydroindole Scaffolds.Organic letters · 2020Article
- S100A10 and Cancer Hallmarks: Structure, Functions, and its Emerging Role in Ovarian Cancer.International journal of molecular sciences · 2018Review
- S100 proteins as therapeutic targets.Biophysical reviews · 2018Review
- Regulation of von-Willebrand Factor Secretion from Endothelial Cells by the Annexin A2-S100A10 Complex.International journal of molecular sciences · 2018Review
- Annexin A2 in Virus Infection.Frontiers in microbiology · 2018Article
- 4-Aroyl-3-hydroxy-5-phenyl-1H-pyrrol-2(5H)-ones as N-formyl peptide receptor 1 (FPR1) antagonists.Biochemical pharmacology · 2017Article
- Stereoselective Synthesis of Quaternary Pyrrolidine-2,3-diones and β-Amino Acids.Organic letters · 2017Article
- Annexin A2 complexes with S100 proteins: structure, function and pharmacological manipulation.British journal of pharmacology · 2015Review
- An integrated biological approach to guide the development of metal-chelating inhibitors of influenza virus PA endonuclease.Molecular pharmacology · 2015Article
- Hierarchical virtual screening approaches in small molecule drug discovery.Methods (San Diego, Calif.) · 2015Review
- Article
- Small molecule inhibitors of the annexin A2 heterotetramer prevent human papillomavirus type 16 infection.The Journal of antimicrobial chemotherapy · 2015Article
- Design, synthesis and SAR exploration of tri-substituted 1,2,4-triazoles as inhibitors of the annexin A2-S100A10 protein interaction.Bioorganic & medicinal chemistry · 2014Article
- Article
- Functions of S100 proteins.Current molecular medicine · 2013Review
- In vivo screening of S100B inhibitors for melanoma therapy.Methods in molecular biology (Clifton, N.J.) · 2013Article
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
S100 proteins are small adaptors that regulate the activity of partner proteins by virtue of direct protein interactions. Here, we describe the first small molecule blockers of the interaction between S100A10 and annexin A2. Molecular docking yielded candidate blockers that were screened for competition of the binding of an annexin A2 peptide to S100A10. Several inhibitory clusters were identified with some containing compounds with potency in the lower micromolar range. We chose 3-hydroxy-1-(2-hydroxypropyl)-5-(4-isopropylphenyl)-4-(4-methylbenzoyl)-1H-pyrrol-2(5H)-one (1a) as a starting point for structure-activity studies. These confirmed the hypothetical binding mode from the virtual screen for this series of molecules. Selected compounds disrupted the physiological complex of annexin A2 and S100A10, both in a broken cell preparation and inside MDA-MB-231 breast cancer cells. Thus, this class of compounds has promising properties as inhibitors of the interaction between annexin A2 and S100A10 and may help to elucidate the cellular function of this protein interaction.
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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.