文章：

维生素A有望对抗癌症

The promise of retinoids to fight against cancer

原文发布日期：2001-12-01

DOI: 10.1038/35106036

类型: Review Article

开放获取: 否

要点：

1. Retinoids and rexinoids exert their action by signalling through nuclear receptor heterodimers that can activate or silence specific gene networks.
2. The most widely studied retinoid, all-trans retinoic acid (ATRA), causes differentiation of acute promyelocytic leukaemia (APL) cells through activation of the retinoid receptor RARα, but RARβ and rexinoid receptors (RXRs) might also be responsible for some of the antitumour activity of retinoids.
3. Crosstalk with other transcription factors, particularly AP1 (FOS–JUN), might account for some of the antitumour activity of retinoids.
4. In humans, pharmacological doses of ATRA cause differentiation of APL cells that contain the PML–RARα fusion protein, but clinical data indicate that retinoids might also be useful for the treatment of other human cancers.
5. As well as activating differentiation, retinoids can also activate tumour-specific death signalling pathways; these contribute to the efficacy of retinoid therapy.
6. Retinoids are cancer preventive and their use has been approved for the treatment of several precancerous conditions.

要点翻译：

1. 类维生素A与类视黄醇通过核受体异源二聚体介导的信号传导发挥作用，这些二聚体可激活或沉默特定基因网络。
2. 研究最广泛的类维生素A——全反式维甲酸（ATRA）通过激活视黄酸受体RARα促使急性早幼粒细胞白血病（APL）细胞分化，但RARβ和类视黄醇X受体（RXR）可能也参与了类维生素A的部分抗肿瘤活性。
3. 与其他转录因子（特别是AP1（FOS-JUN复合物））的交叉对话可能是类维生素A发挥抗肿瘤作用的机制之一。
4. 在人体中，药理学剂量的ATRA可诱导含有PML-RARα融合蛋白的APL细胞分化，但临床数据表明类维生素A也可能适用于其他人类癌症的治疗。
5. 除激活分化外，类维生素A还能激活肿瘤特异性死亡信号通路，这些通路共同增强了类维生素A疗法的疗效。
6. 类维生素A具有癌症预防作用，目前已获准用于多种癌前病变的治疗。

英文摘要：

Retinoids have a reputation for being both detrimental and beneficial: they are teratogens, but they also have tumour-suppressive capacity. Cell biology and genetics have significantly improved our understanding of the mechanisms that underlie the anti-proliferative action of retinoids. Recent elucidation of the pathways that are activated by retinoids will help us to exploit the beneficial aspects of this powerful class of compounds for cancer therapy and prevention.

摘要翻译： 

类维生素A类物质具有双重声誉：既具有危害性，也具益处——它们是致畸物，但同时也拥有抑制肿瘤的能力。细胞生物学和遗传学显著增进了我们对类维生素A抗增殖作用机制的理解。近期对其激活通路的阐明，将有助于我们利用这类强效化合物的有益特性，为癌症治疗和预防开辟新途径。

原文链接：

The promise of retinoids to fight against cancer