Kovač Urša, Skubic Cene, Bohinc Laura, Rozman Damjana, Režen Tadeja
Centre for Functional Genomics and Bio-Chips, Institute of Biochemistry, Faculty of Medicine, University of Ljubljana, Ljubljana, Slovenia.
Front Endocrinol (Lausanne). 2019 Jul 17;10:483. doi: 10.3389/fendo.2019.00483. eCollection 2019.
This review focuses on the role of oxidized sterols in three major gastrointestinal cancers (hepatocellular carcinoma, pancreatic, and colon cancer) and how the circadian clock affects the carcinogenesis by regulating the lipid metabolism and beyond. While each field of research (cancer, oxysterols, and circadian clock) is well-studied within their specialty, little is known about the intertwining mechanisms and how these influence the disease etiology in each cancer type. Oxysterols are involved in pathology of these cancers, but final conclusions about their protective or damaging effects are elusive, since the effect depends on the type of oxysterol, concentration, and the cell type. Oxysterol concentrations, the expression of key regulators liver X receptors (LXR), farnesoid X receptor (FXR), and oxysterol-binding proteins (OSBP) family are modulated in tumors and plasma of cancer patients, exposing these proteins and selected oxysterols as new potential biomarkers and drug targets. Evidence about how cholesterol/oxysterol pathways are intertwined with circadian clock is building. Identified key contact points are different forms of retinoic acid receptor related orphan receptors (ROR) and LXRs. RORs and LXRs are both regulated by sterols/oxysterols and the circadian clock and in return also regulate the same pathways, representing a complex interplay between sterol metabolism and the clock. With this in mind, in addition to classical therapies to modulate cholesterol in gastrointestinal cancers, such as the statin therapy, the time is ripe also for therapies where time and duration of the drug application is taken as an important factor for successful therapies. The final goal is the personalized approach with chronotherapy for disease management and treatment in order to increase the positive drug effects.
本综述聚焦于氧化甾醇在三种主要胃肠道癌症(肝细胞癌、胰腺癌和结肠癌)中的作用,以及生物钟如何通过调节脂质代谢及其他方面影响癌症发生。虽然每个研究领域(癌症、氧化甾醇和生物钟)在其专业范围内都有深入研究,但对于它们相互交织的机制以及这些机制如何影响每种癌症类型的疾病病因却知之甚少。氧化甾醇参与了这些癌症的病理过程,但关于它们的保护或损害作用的最终结论尚难以确定,因为其作用取决于氧化甾醇的类型、浓度和细胞类型。癌症患者肿瘤和血浆中的氧化甾醇浓度、关键调节因子肝脏X受体(LXR)、法尼醇X受体(FXR)和氧化甾醇结合蛋白(OSBP)家族的表达均受到调节,这使得这些蛋白质和特定氧化甾醇成为新的潜在生物标志物和药物靶点。关于胆固醇/氧化甾醇途径与生物钟如何相互交织的证据正在不断积累。已确定的关键接触点是不同形式的视黄酸受体相关孤儿受体(ROR)和LXR。ROR和LXR均受甾醇/氧化甾醇和生物钟调节,反过来也调节相同的途径,这代表了甾醇代谢与生物钟之间的复杂相互作用。考虑到这一点,除了在胃肠道癌症中调节胆固醇的经典疗法(如他汀类药物疗法)外,将药物应用的时间和持续时间作为成功治疗的重要因素的疗法时机也已成熟。最终目标是采用时辰疗法进行个性化疾病管理和治疗,以增强药物的积极效果。