title: Flavonoids as inhibitors of human CD38.
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 Ca(2+) 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 (IC(50) <10 μM). Docking studies provide some clues on the mode of interaction of these molecules with the active site of CD38.
authors.affiliation: Laboratoire d'Innovation Thérapeutique, UMR 7200 CNRS-Université de Strasbourg, Faculté de Pharmacie, 74 route du Rhin, 67400 Illkirch, France.
authors.forename: Esther
authors.initials: E
authors.lastname: Kellenberger
authors.forename: Isabelle
authors.initials: I
authors.lastname: Kuhn
authors.forename: Francis
authors.initials: F
authors.lastname: Schuber
authors.forename: Hélène
authors.initials: H
authors.lastname: Muller-Steffner
mesh_terms: D051997:ADP-ribosyl Cyclase 1 / Q000037:antagonists & inhibitors*; D000872:Anthocyanins / Q000737:chemistry / Q000494:pharmacology; D020134:Catalytic Domain; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D015394:Molecular Structure
chemical_list: D000872:Anthocyanins; D004791:Enzyme Inhibitors; D005419:Flavonoids; D051997:ADP-ribosyl Cyclase 1; C518537:luteolinidin