title: 4-[3-(5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)phenyl]benzoic acid and heterocyclic-bridged analogues are novel retinoic acid receptor subtype and retinoid X receptor alpha agonists.
abstract: Aromatic retinoids having a meta-substituted aromatic ring bridge, such as 4-[3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)phenyl]benzo ic acid and its 3,5-diaryl-substituted 4,5-dihydroisoxazole analogue, function as retinoid receptor panagonists by activating both retinoic acid and retinoid X receptors to induce gene transcription, and thereby provide novel scaffolds for retinoid drug development. Both classes of these ligand-inducible transcription factors are involved in mediating the inhibitory effects of retinoids on cancer cell growth.
authors.affiliation: Medicinal Chemistry Department, Molecular Medicine Research Institute, Mountain View, CA 94043, USA. mdawson@mmrx.org
authors.forename: M I
authors.initials: MI
authors.lastname: Dawson
authors.forename: L
authors.initials: L
authors.lastname: Jong
authors.forename: P D
authors.initials: PD
authors.lastname: Hobbs
authors.forename: D
authors.initials: D
authors.lastname: Xiao
authors.forename: K C
authors.initials: KC
authors.lastname: Feng
authors.forename: W R
authors.initials: WR
authors.lastname: Chao
authors.forename: C
authors.initials: C
authors.lastname: Pan
authors.forename: J A
authors.initials: JA
authors.lastname: Fontana
authors.forename: X K
authors.initials: XK
authors.lastname: Zhang
mesh_terms: D001565:Benzoates / Q000737:chemistry / Q000494:pharmacology*; D006571:Heterocyclic Compounds / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D009281:Naphthalenes / Q000737:chemistry / Q000494:pharmacology*; D018168:Receptors, Retinoic Acid / Q000819:agonists*; D047488:Retinoid X Receptors; D014157:Transcription Factors / Q000819:agonists*; D014407:Tumor Cells, Cultured
chemical_list: C415643:4-(3-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)phenyl)benzoic acid; D001565:Benzoates; D006571:Heterocyclic Compounds; D009281:Naphthalenes; D018168:Receptors, Retinoic Acid; D047488:Retinoid X Receptors; D014157:Transcription Factors