retinoid-related抗肿瘤活性分子(E) 3 - (4 ' -hydroxy-3 ' -adamantylbiphenyl-4-yl)丙烯酸(ST1926)和6 - [3 - (1-adamantyl) 4-hydroxyphenyl] 2-naphthalene羧酸(CD437) F9畸胎癌:视黄酸受体γ和retinoid-independent通路的作用。

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Parrella E,詹尼·M,全片M, Barzago MM,声明我小,Diomede L, Kurosaki M,皮萨诺C, Carminati P, Merlini L, Dallavalle年代,Tavecchio M, Rochette-Egly C, Terao M, Garattini E

摩尔杂志。2006年9月,70 (3):909 - 24。Epub 2006 6月20。

PubMed ID

16788091 (在PubMed

]

文摘

retinoid-related分子(名RRMs) ST1926 [(E) 3 - (4 ' -hydroxy-3 ' -adamantylbiphenyl-4-yl)丙烯酸)和CD437 (6 - [3 - (1-adamantyl) 4-hydroxyphenyl] 2-naphthalene羧酸)是有前途的抗癌剂。我们比较了视黄酸受体(RAR)两名RRMs trans-activating属性和all-trans-retinoic酸(ATRA)。ST1926和CD437比ATRA RARgamma受体激动剂。我们使用三个畸胎癌细胞系评估的意义活动名RRMs RARgamma: F9-wild类型(WT);F9gamma - / -,缺乏RARgamma基因;F9gamma51 aF9gamma——/导数,补充RARgamma赤字。类似于ATRA ST1926 CD437激活只在F9-WT cytodifferentiation细胞。与ATRA不同,ST1926和CD437逮捕细胞G2 / M期细胞周期和诱导细胞凋亡F9细胞系。我们的数据表明,RARgamma和经典类维生素a通路不相关的抗增殖和凋亡活动名RRMs体外。增加胞质钙是细胞凋亡的根本,在细胞内钙螯合剂废除这一过程。 Comparison of the gene expression profiles associated with ST1926 and ATRA in F9-WT and F9gamma-/-indicates that the RRM activates a conspicuous nonretinoid response in addition to the classic and RAR-dependent pathway. The pattern of genes regulated by ST1926 selectively, in a RARgamma-independent manner, provides novel insights into the possible molecular determinants underlying the activity of RRMs in vitro. Furthermore, it suggests that RARgamma-dependent responses are relevant to the activity of RRMs in vivo. Indeed, the receptor hinders the antitumor activity in vivo, in that both syngeneic and immunosuppressed SCID mice bearing F9gamma-/- tumors have increased life spans after treatment with ST1926 and CD437 relative to their F9-WT counterparts.

DrugBank数据引用了这篇文章

药物靶点

药物	目标	类	生物	药理作用	行动
Alitretinoin	视黄酸受体γ	蛋白质	人类	是的	受体激动剂	细节