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doi:10.22028/D291-39085
Titel: | 7-Hydroxycoumarins Are Affinity-Based Fluorescent Probes for Competitive Binding Studies of Macrophage Migration Inhibitory Factor |
VerfasserIn: | Xiao, Zhangping Chen, Deng Song, Shanshan van der Vlag, Ramon van der Wouden, Petra E. van Merkerk, Ronald Cool, Robbert H. Hirsch, Anna K. H. Melgert, Barbro N. Quax, Wim J. Poelarends, Gerrit J. Dekker, Frank J. |
Sprache: | Englisch |
Titel: | Journal of Medicinal Chemistry |
Bandnummer: | 63 |
Heft: | 20 |
Seiten: | 11920-11933 |
Verlag/Plattform: | American Chemical Society |
Erscheinungsjahr: | 2020 |
Freie Schlagwörter: | Assays Fluorescence Imaging probes Inhibitors Peptides and proteins |
DDC-Sachgruppe: | 500 Naturwissenschaften |
Dokumenttyp: | Journalartikel / Zeitschriftenartikel |
Abstract: | Macrophage migration inhibitory factor (MIF) is a cytokine with key roles in inflammation and cancer, which qualifies it as a potential drug target. Apart from its cytokine activity, MIF also harbors enzyme activity for keto−enol tautomerization. MIF enzymatic activity has been used for identification of MIF binding molecules that also interfere with its biological activity. However, MIF tautomerase activity assays are troubled by irregularities, thus creating a need for alternative methods. In this study, we identified a 7-hydroxycoumarin fluorophore with high affinity for the MIF tautomerase active site (Ki = 18 ± 1 nM) that binds with concomitant quenching of its fluorescence. This property enabled development of a novel competitionbased assay format to quantify MIF binding. We also demonstrated that the 7-hydroxycoumarin fluorophore interfered with the MIF−CD74 interaction and inhibited proliferation of A549 cells. Thus, we provide a high-affinity MIF binder as a novel tool to advance MIF-oriented research. |
DOI der Erstveröffentlichung: | 10.1021/acs.jmedchem.0c01160 |
URL der Erstveröffentlichung: | https://pubs.acs.org/doi/10.1021/acs.jmedchem.0c01160 |
Link zu diesem Datensatz: | urn:nbn:de:bsz:291--ds-390857 hdl:20.500.11880/35244 http://dx.doi.org/10.22028/D291-39085 |
ISSN: | 1520-4804 |
Datum des Eintrags: | 17-Feb-2023 |
Bezeichnung des in Beziehung stehenden Objekts: | Supporting Information |
In Beziehung stehendes Objekt: | https://pubs.acs.org/doi/suppl/10.1021/acs.jmedchem.0c01160/suppl_file/jm0c01160_si_001.pdf https://pubs.acs.org/doi/suppl/10.1021/acs.jmedchem.0c01160/suppl_file/jm0c01160_si_002.csv https://pubs.acs.org/doi/suppl/10.1021/acs.jmedchem.0c01160/suppl_file/jm0c01160_si_003.pdb |
Fakultät: | NT - Naturwissenschaftlich- Technische Fakultät |
Fachrichtung: | NT - Pharmazie |
Professur: | NT - Prof. Dr. Anna Hirsch |
Sammlung: | SciDok - Der Wissenschaftsserver der Universität des Saarlandes |
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