title: A novel atypical retinoid endowed with proapoptotic and antitumor activity.
abstract: The novel atypical retinoid E-3-(4'-hydroxy-3'-adamantylbiphenyl-4-yl)acrylic acid (ST1926, 4) exhibited a potent antiproliferative activity on a large panel of human tumor cells. Despite almost complete loss of ability to activate RARs, the compound was an effective apoptosis inducer and surprisingly produced DNA damage, that likely contributes to the proapoptotic activity. Following oral administration, 4 was well tolerated and caused tumor growth inhibition in the ovarian carcinoma, A2780/DX, and in the human melanoma, MeWo, growing in nude mice, thus supporting the therapeutic interest of the novel agent.
authors.affiliation: Dipartimento di Scienze Molecolari Agroalimentari, Università di Milano, Milano, Italy.
authors.forename: Raffaella
authors.initials: R
authors.lastname: Cincinelli
authors.forename: Sabrina
authors.initials: S
authors.lastname: Dallavalle
authors.forename: Lucio
authors.initials: L
authors.lastname: Merlini
authors.forename: Sergio
authors.initials: S
authors.lastname: Penco
authors.forename: Claudio
authors.initials: C
authors.lastname: Pisano
authors.forename: Paolo
authors.initials: P
authors.lastname: Carminati
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Giannini
authors.forename: Loredana
authors.initials: L
authors.lastname: Vesci
authors.forename: Carlo
authors.initials: C
authors.lastname: Gaetano
authors.forename: Barbara
authors.initials: B
authors.lastname: Illy
authors.forename: Valentina
authors.initials: V
authors.lastname: Zuco
authors.forename: Rosanna
authors.initials: R
authors.lastname: Supino
authors.forename: Franco
authors.initials: F
authors.lastname: Zunino
mesh_terms: D000218:Adamantane / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis; D002934:Cinnamates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004249:DNA Damage; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D008545:Melanoma / Q000188:drug therapy / Q000473:pathology; D051379:Mice; D008819:Mice, Nude; D010051:Ovarian Neoplasms / Q000188:drug therapy / Q000473:pathology; D020033:Protein Isoforms; D018168:Receptors, Retinoic Acid / Q000235:genetics / Q000378:metabolism; D012176:Retinoids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014162:Transfection; D014183:Transplantation, Heterologous; D014407:Tumor Cells, Cultured
chemical_list: C472791:3-(4'-hydroxy-3'-adamantylbiphenyl-4-yl)acrylic acid; D000970:Antineoplastic Agents; D002934:Cinnamates; D020033:Protein Isoforms; D018168:Receptors, Retinoic Acid; D012176:Retinoids; D000218:Adamantane