title: Modulation of proteasome machinery by natural and synthetic analogues of the marine bioactive compound petrosaspongiolide M.
abstract: Natural or synthetic? Several petrosaspongiolide M natural and synthetic analogues have been tested as proteasome inhibitors and apoptosis modulators. The natural petrosaspongiolide M congeners gave a consistent decrease in activity. Among the synthetic analogues, the introduction of the benzothiophene ring resulted in a bioequivalent alternative of the petrosaspongiolide M terpenoid system.
authors.affiliation: Department of Pharmaceutical and Biomedical Sciences, University of Salerno, Via Ponte don Melillo, 84084 Fisciano, Italy.
authors.forename: Luigi
authors.initials: L
authors.lastname: Margarucci
authors.forename: Alessandra
authors.initials: A
authors.lastname: Tosco
authors.forename: Rosa
authors.initials: R
authors.lastname: De Simone
authors.forename: Raffaele
authors.initials: R
authors.lastname: Riccio
authors.forename: Maria Chiara
authors.initials: MC
authors.lastname: Monti
authors.forename: Agostino
authors.initials: A
authors.lastname: Casapullo
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D005470:Fluorometry; D006801:Humans; D009828:Oleanolic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D010741:Phospholipases A / Q000037:antagonists & inhibitors*; D011161:Porifera; D061988:Proteasome Inhibitors; D013329:Structure-Activity Relationship; D020298:U937 Cells
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D061988:Proteasome Inhibitors; C118309:petrosaspongiolide m; D009828:Oleanolic Acid; D010741:Phospholipases A