Flavonoids as inhibitors of human CD38 |
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Authors: | Kellenberger Esther Kuhn Isabelle Schuber Francis Muller-Steffner Hélène |
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Affiliation: | a Laboratoire d’Innovation Thérapeutique, UMR 7200 CNRS—Université de Strasbourg, Faculté de Pharmacie, 74 route du Rhin, 67400 Illkirch, France b Laboratoire de Conception et Application de Molécules Bioactives, UMR 7199 CNRS—Université de Strasbourg, Faculté de Pharmacie, 74 route du Rhin, 67400 Illkirch, France |
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Abstract: | CD38 is a multifunctional enzyme which is ubiquitously distributed in mammalian tissues. It is involved in the conversion of NAD(P)+ into cyclic ADP-ribose, NAADP+ and ADP-ribose and the role of these metabolites in multiple Ca2+ signaling pathways makes CD38 a novel potential pharmacological target. The dire paucity of CD38 inhibitors, however, renders the search for new molecular tools highly desirable. We report that human CD38 is inhibited at low micromolar concentrations by flavonoids such as luteolinidin, kuromanin and luteolin (IC50 <10 μM). Docking studies provide some clues on the mode of interaction of these molecules with the active site of CD38. |
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Keywords: | CD38 Flavonoids Anthocyanidins Inhibition Docking |
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