ArticleBioorganic & medicinal chemistry letters2010
Optimization of N-benzyl-benzoxazol-2-ones as receptor antagonists of macrophage migration inhibitory factor (MIF).
Article in Bioorganic & medicinal chemistry letters, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers.
What it found
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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.
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Who cites it
34 citing papers in PubMed, 63 citations in OpenAlex.
- MIF contribution to progressive brain diseases.Journal of neuroinflammation · 2024Review
- Article
- The N-terminus of MIF regulates the dynamic profile of residues involved in CD74 activation.Biophysical journal · 2021Article
- Intravesical CD74 and CXCR4, macrophage migration inhibitory factor (MIF) receptors, mediate bladder pain.PloS one · 2021Article
- The road ahead for health and lifespan interventions.Ageing research reviews · 2020Review
- Glioblastoma Myeloid-Derived Suppressor Cell Subsets Express Differential Macrophage Migration Inhibitory Factor Receptor Profiles That Can Be Targeted to Reduce Immune Suppression.Frontiers in immunology · 2020Article
- A selective small-molecule inhibitor of macrophage migration inhibitory factor-2 (MIF-2), a MIF cytokine superfamily member, inhibits MIF-2 biological activity.The Journal of biological chemistry · 2019Article
- Novel Role of Macrophage Migration Inhibitory Factor in Upstream Control of the Unfolded Protein Response After Ethanol Feeding in Mice.Alcoholism, clinical and experimental research · 2019Article
- The immunobiology of MIF: function, genetics and prospects for precision medicine.Nature reviews. Rheumatology · 2019Review
- MIF family proteins in genitourinary cancer: tumorigenic roles and therapeutic potential.Nature reviews. Urology · 2019Review
- Endothelial cell-secreted MIF reduces pericyte contractility and enhances neutrophil extravasation.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2019Article
- Small-molecule inhibitors of macrophage migration inhibitory factor (MIF) as an emerging class of therapeutics for immune disorders.Drug discovery today · 2018Review
- Advances and Insights for Small Molecule Inhibition of Macrophage Migration Inhibitory Factor.Journal of medicinal chemistry · 2018Article
- Optimization of Pyrazoles as Phenol Surrogates to Yield Potent Inhibitors of Macrophage Migration Inhibitory Factor.ChemMedChem · 2018Article
- Review
- Interaction Between Macrophage Migration Inhibitory Factor and CD74 in Human Immunodeficiency Virus Type I Infected Primary Monocyte-Derived Macrophages Triggers the Production of Proinflammatory Mediators and Enhances Infection of Unactivated CD4Frontiers in immunology · 2018Article
- MIF family cytokines in cardiovascular diseases and prospects for precision-based therapeutics.Expert opinion on therapeutic targets · 2017Review
- The biological function and significance of CD74 in immune diseases.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2017Review
- MIF allele-dependent regulation of the MIF coreceptor CD44 and role in rheumatoid arthritis.Proceedings of the National Academy of Sciences of the United States of America · 2016Article
- Structure-based predictions of activity cliffs.Journal of chemical information and modeling · 2015Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
The cytokine MIF is involved in inflammation and cell proliferation via pathways initiated by its binding to the transmembrane receptor CD74. MIF also exhibits keto-enol tautomerase activity, believed to be vestigial in mammals. Starting from a 1 μM hit from virtual screening, substituted benzoxazol-2-ones have been discovered as antagonists with IC(50) values as low as 7.5 nM in a tautomerase assay and 80 nM in a MIF-CD74 binding assay. Additional studies for one of the potent inhibitors demonstrated that it is not a covalent inhibitor of MIF and that it attenuates MIF-dependent ERK1/2 phosphorylation in human synovial fibroblasts.
Indexed as
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What OpenQuestion 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 OpenQuestion graph.