Literature DB >> 27739690

Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.

Melania Olivieri1, Emanuele Amata2, Shila Vinciguerra2, Jole Fiorito2, Giovanni Giurdanella1, Filippo Drago1, Nunzia Caporarello1, Orazio Prezzavento2, Emanuela Arena2, Loredana Salerno2, Antonio Rescifina2, Gabriella Lupo1, Carmelina Daniela Anfuso1, Agostino Marrazzo2.   

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.

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Year:  2016        PMID： 27739690     DOI： 10.1021/acs.jmedchem.6b01039

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  12 in total

1.  Sigma Receptor Ligands Carrying a Nitric Oxide Donor Nitrate Moiety: Synthesis, In Silico, and Biological Evaluation.

Authors:  Emanuele Amata; Maria Dichiara; Davide Gentile; Agostino Marrazzo; Rita Turnaturi; Emanuela Arena; Alfonsina La Mantia; Barbara Rita Tomasello; Rosaria Acquaviva; Claudia Di Giacomo; Antonio Rescifina; Orazio Prezzavento
Journal:  ACS Med Chem Lett       Date:  2020-04-09       Impact factor: 4.345

Review 2.  Sigmar1's Molecular, Cellular, and Biological Functions in Regulating Cellular Pathophysiology.

Authors:  Richa Aishwarya; Chowdhury S Abdullah; Mahboob Morshed; Naznin Sultana Remex; Md Shenuarin Bhuiyan
Journal:  Front Physiol       Date:  2021-07-07       Impact factor: 4.566

3.  Sigma-1 and Sigma-2 receptor ligands induce apoptosis and autophagy but have opposite effect on cell proliferation in uveal melanoma.

Authors:  Lucia Longhitano; Carlo Castruccio Castracani; Daniele Tibullo; Roberto Avola; Maria Viola; Giuliano Russo; Orazio Prezzavento; Agostino Marrazzo; Emanuele Amata; Michele Reibaldi; Antonio Longo; Andrea Russo; Nunziatina Laura Parrinello; Giovanni Li Volti
Journal:  Oncotarget       Date:  2017-07-25

4.  S2RSLDB: a comprehensive manually curated, internet-accessible database of the sigma-2 receptor selective ligands.

Authors:  Giovanni Nastasi; Carla Miceli; Valeria Pittalà; Maria N Modica; Orazio Prezzavento; Giuseppe Romeo; Antonio Rescifina; Agostino Marrazzo; Emanuele Amata
Journal:  J Cheminform       Date:  2017-01-21       Impact factor: 5.514

5.  In Vitro Antioxidant Activity of Idebenone Derivative-Loaded Solid Lipid Nanoparticles.

Authors:  Lucia Montenegro; Maria N Modica; Loredana Salerno; Anna Maria Panico; Lucia Crascì; Giovanni Puglisi; Giuseppe Romeo
Journal:  Molecules       Date:  2017-05-27       Impact factor: 4.411

6.  A Structure- and Ligand-Based Virtual Screening of a Database of "Small" Marine Natural Products for the Identification of "Blue" Sigma-2 Receptor Ligands.

Authors:  Giuseppe Floresta; Emanuele Amata; Carla Barbaraci; Davide Gentile; Rita Turnaturi; Agostino Marrazzo; Antonio Rescifina
Journal:  Mar Drugs       Date:  2018-10-14       Impact factor: 5.118

7.  Anti-angiogenic effect of quercetin and its 8-methyl pentamethyl ether derivative in human microvascular endothelial cells.

Authors:  Gabriella Lupo; Maria Teresa Cambria; Melania Olivieri; Concetta Rocco; Nunzia Caporarello; Anna Longo; Guido Zanghì; Mario Salmeri; Mario C Foti; Carmelina Daniela Anfuso
Journal:  J Cell Mol Med       Date:  2019-08-01       Impact factor: 5.310

8.  Haloperidol Induced Cell Cycle Arrest and Apoptosis in Glioblastoma Cells.

Authors:  Fotios Papadopoulos; Rafaela Isihou; George A Alexiou; Thomas Tsalios; Evrysthenis Vartholomatos; Georgios S Markopoulos; Chrissa Sioka; Pericles Tsekeris; Athanasios P Kyritsis; Vasiliki Galani
Journal:  Biomedicines       Date:  2020-12-11

9.  NO1, a New Sigma 2 Receptor/TMEM97 Fluorescent Ligand, Downregulates SOCE and Promotes Apoptosis in the Triple Negative Breast Cancer Cell Lines.

Authors:  Carlos Cantonero; Pedro Javier Camello; Carmen Abate; Francesco Berardi; Gines Maria Salido; Juan Antonio Rosado; Pedro C Redondo
Journal:  Cancers (Basel)       Date:  2020-01-21       Impact factor: 6.639

10.  Nitric Oxide Photo-Donor Hybrids of Ciprofloxacin and Norfloxacin: A Shift in Activity from Antimicrobial to Anticancer Agents.

Authors:  Antonino Nicolò Fallica; Carla Barbaraci; Emanuele Amata; Lorella Pasquinucci; Rita Turnaturi; Maria Dichiara; Sebastiano Intagliata; Marzia Bruna Gariboldi; Emanuela Marras; Viviana Teresa Orlandi; Claudia Ferroni; Cecilia Martini; Antonio Rescifina; Davide Gentile; Greta Varchi; Agostino Marrazzo
Journal:  J Med Chem       Date:  2021-07-28       Impact factor: 8.039
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