title: Chemical inhibitors of monogalactosyldiacylglycerol synthases in Arabidopsis thaliana.
abstract: Monogalactosyldiacylglycerol (MGDG) and digalactosyldiacylglycerol (DGDG) are the main lipids in photosynthetic membranes in plant cells. They are synthesized in the envelope surrounding plastids by MGD and DGD galactosyltransferases. These galactolipids are critical for the biogenesis of photosynthetic membranes, and they act as a source of polyunsaturated fatty acids for the whole cell and as phospholipid surrogates in phosphate shortage. Based on a high-throughput chemical screen, we have characterized a new compound, galvestine-1, that inhibits MGDs in vitro by competing with diacylglycerol binding. Consistent effects of galvestine-1 on Arabidopsis thaliana include root uptake, circulation in the xylem and mesophyll, inhibition of MGDs in vivo causing a reduction of MGDG content and impairment of chloroplast development. The effects on pollen germination shed light on the contribution of galactolipids to pollen-tube elongation. The whole-genome transcriptional response of Arabidopsis points to the potential benefits of galvestine-1 as a unique tool to study lipid homeostasis in plants.
authors.affiliation: Commissariat à l'Energie Atomique, Centre National de la Recherche Scientifique, Université Joseph Fourier Grenoble I, Institut National de la Recherche Agronomique, Unité Mixte de Recherche 5168, Grenoble, France.
authors.forename: Cyrille Y
authors.initials: CY
authors.lastname: Botté
authors.forename: Michael
authors.initials: M
authors.lastname: Deligny
authors.forename: Aymeric
authors.initials: A
authors.lastname: Roccia
authors.forename: Anne-Laure
authors.initials: AL
authors.lastname: Bonneau
authors.forename: Nadia
authors.initials: N
authors.lastname: Saïdani
authors.forename: Hélène
authors.initials: H
authors.lastname: Hardré
authors.forename: Samia
authors.initials: S
authors.lastname: Aci
authors.forename: Yoshiki
authors.initials: Y
authors.lastname: Yamaryo-Botté
authors.forename: Juliette
authors.initials: J
authors.lastname: Jouhet
authors.forename: Emmanuelle
authors.initials: E
authors.lastname: Dubots
authors.forename: Karen
authors.initials: K
authors.lastname: Loizeau
authors.forename: Olivier
authors.initials: O
authors.lastname: Bastien
authors.forename: Laurent
authors.initials: L
authors.lastname: Bréhélin
authors.forename: Jacques
authors.initials: J
authors.lastname: Joyard
authors.forename: Jean-Christophe
authors.initials: JC
authors.lastname: Cintrat
authors.forename: Denis
authors.initials: D
authors.lastname: Falconet
authors.forename: Maryse A
authors.initials: MA
authors.lastname: Block
authors.forename: Bernard
authors.initials: B
authors.lastname: Rousseau
authors.forename: Roman
authors.initials: R
authors.lastname: Lopez
authors.forename: Eric
authors.initials: E
authors.lastname: Maréchal
mesh_terms: D017360:Arabidopsis / Q000201:enzymology*; D004791:Enzyme Inhibitors / Q000494:pharmacology; D038983:Galactolipids / Q000378:metabolism; D005700:Galactosyltransferases / Q000037:antagonists & inhibitors*; D020869:Gene Expression Profiling; D015971:Gene Expression Regulation, Enzymologic / Q000187:drug effects*; D018506:Gene Expression Regulation, Plant / Q000187:drug effects*; D015394:Molecular Structure; D010880:Piperidines / Q000494:pharmacology; D018515:Plant Leaves / Q000648:ultrastructure; D018517:Plant Roots / Q000378:metabolism; D054852:Small Molecule Libraries; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D038983:Galactolipids; D010880:Piperidines; D054852:Small Molecule Libraries; C007388:digalactosyldiacylglycerol; C568628:galvestine-1; C009909:monogalactosyldiacylglycerol; D005700:Galactosyltransferases; C109990:1,2-diacylglycerol 3-beta-galactosyltransferase