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4-[3-(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)苯基]苯甲酸及其杂环桥连类似物是新型维甲酸受体亚型和维甲酸X受体α激动剂。

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.

作者信息

Dawson M I, Jong L, Hobbs P D, Xiao D, Feng K C, Chao W R, Pan C, Fontana J A, Zhang X K

机构信息

Medicinal Chemistry Department, Molecular Medicine Research Institute, Mountain View, CA 94043, USA.

出版信息

Bioorg Med Chem Lett. 2000 Jun 19;10(12):1311-3. doi: 10.1016/s0960-894x(00)00244-4.

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.

摘要

具有间位取代芳环桥的芳香族维甲酸,如4-[3-(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)苯基]苯甲酸及其3,5-二芳基取代的4,5-二氢异恶唑类似物,通过激活视黄酸受体和视黄醇X受体来诱导基因转录,从而作为维甲酸受体泛激动剂发挥作用,进而为维甲酸药物开发提供了新的骨架。这两类配体诱导型转录因子都参与介导维甲酸对癌细胞生长的抑制作用。

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