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Oxysterol receptors and their therapeutic applications in cancer conditions

机译:氧固醇受体及其在癌症中的治疗应用

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Introduction: Oxysterols are implicated in various cellular processes. Among their target proteins, liver X receptors (LXRs) α and β modulate the cell cycle in a large range of cancer cell lines. Besides their role as cholesterol sensors, LXRs are also involved in the proliferation/ apoptosis balance regulation in various types of cancers. Areas covered: This review covers oxysterols and derivatives of cholesterol as well as synthetic or natural ligands (agonist/antagonist) of LXRs. Most tumor cell lines are sensitive to LXR activation. Indeed various cancers are concerned such as prostate, breast, glioblastoma, colorectal, and ovary tumors, and leukemia. Expert opinion: Developing the use of LXR ligands in human health, especially in the field of cancer, represents a novel and promising strategy. Despite a wide spectrum of applications, numerous adverse effects of LXR activation need to be solved before genuine clinical trials in humans. Future directions will be based on the engineering of selective LXRs modulators (SLiMs) as already done for nuclear steroid receptors.
机译:简介:氧固醇与各种细胞过程有关。在它们的靶蛋白中,肝X受体(LXR)α和β可以调节多种癌细胞系的细胞周期。除了其作为胆固醇传感器的作用外,LXR还参与各种类型癌症的增殖/凋亡平衡调节。涵盖的领域:该综述涵盖氧固醇和胆固醇衍生物以及LXR的合成或天然配体(激动剂/拮抗剂)。大多数肿瘤细胞系对LXR激活敏感。实际上,涉及各种癌症,例如前列腺癌,乳腺癌,成胶质细胞瘤,结肠直肠癌和卵巢癌以及白血病。专家意见:在人类健康(尤其是在癌症领域)中开发LXR配体的使用代表了一种新颖而有希望的战略。尽管应用范围很广,但是在人类进行真正的临床试验之前,需要解决LXR激活的许多不利影响。未来的方向将基于对核甾体受体已经完成的选择性LXR调节剂(SLiMs)的工程设计。

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