title: Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.
abstract: (±)-MRJF22 [(±)-2], a novel prodrug of haloperidol metabolite II (sigma-1 receptor antagonist/sigma-2 receptor agonist ligand) obtained by conjugation to valproic acid (histone deacetylase inhibitor) via an ester bond, exhibits antiangiogenic activity, being able to reduce human retinal endothelial cell (HREC) viability in a comparable manner to bevacizumab. Moreover, (±)-2 was able to significantly reduce viable cells count, endothelial cell migration, and tube formation in vascular endothelial growth factor A (VEGF-A) stimulated HREC cultures.
authors.affiliation: Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania , Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Melania
authors.initials: M
authors.lastname: Olivieri
authors.affiliation: Department of Drug Sciences, University of Catania , Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Emanuele
authors.initials: E
authors.lastname: Amata
authors.affiliation: Department of Drug Sciences, University of Catania , Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Shila
authors.initials: S
authors.lastname: Vinciguerra
authors.affiliation: Department of Drug Sciences, University of Catania , Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Jole
authors.initials: J
authors.lastname: Fiorito
authors.affiliation: Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania , Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Giovanni
authors.initials: G
authors.lastname: Giurdanella
authors.affiliation: Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania , Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Filippo
authors.initials: F
authors.lastname: Drago
authors.affiliation: Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania , Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Nunzia
authors.initials: N
authors.lastname: Caporarello
authors.affiliation: Department of Drug Sciences, University of Catania , Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Orazio
authors.initials: O
authors.lastname: Prezzavento
authors.affiliation: Department of Drug Sciences, University of Catania , Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Emanuela
authors.initials: E
authors.lastname: Arena
authors.affiliation: Department of Drug Sciences, University of Catania , Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Loredana
authors.initials: L
authors.lastname: Salerno
authors.affiliation: Department of Drug Sciences, University of Catania , Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Antonio
authors.initials: A
authors.lastname: Rescifina
authors.affiliation: Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania , Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Gabriella
authors.initials: G
authors.lastname: Lupo
authors.affiliation: Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania , Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Carmelina Daniela
authors.initials: CD
authors.lastname: Anfuso
authors.affiliation: Department of Drug Sciences, University of Catania , Viale A. Doria 6, 95125 Catania, Italy.
authors.forename: Agostino
authors.initials: A
authors.lastname: Marrazzo
mesh_terms: D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D042783:Endothelial Cells / Q000166:cytology / Q000187:drug effects*; D006220:Haloperidol / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D055806:Microvessels / Q000187:drug effects*; D015394:Molecular Structure; D018919:Neovascularization, Physiologic / Q000187:drug effects*; D012160:Retina / Q000166:cytology*; D013329:Structure-Activity Relationship; D014635:Valproic Acid / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D020533:Angiogenesis Inhibitors; D014635:Valproic Acid; D006220:Haloperidol