Girisa Sosmitha, Henamayee Sahu, Parama Dey, Rana Varsha, Dutta Uma, Kunnumakkara Ajaikumar B
Department of Biosciences and Bioengineering, Cancer Biology Laboratory and DBT-AIST International Center for Translational and Environmental Research (DAICENTER), Indian Institute of Technology Guwahati, Guwahati, Assam, 781039, India.
Cell and Molecular Biology Lab, Department of Zoology, Cotton University, Guwahati, Assam, 781001, India.
Mol Biomed. 2021 Jul 10;2(1):21. doi: 10.1186/s43556-021-00035-2.
Cancer is one of the lethal diseases that arise due to the molecular alterations in the cell. One of those alterations associated with cancer corresponds to differential expression of Farnesoid X receptor (FXR), a nuclear receptor regulating bile, cholesterol homeostasis, lipid, and glucose metabolism. FXR is known to regulate several diseases, including cancer and cardiovascular diseases, the two highly reported causes of mortality globally. Recent studies have shown the association of FXR overexpression with cancer development and progression in different types of cancers of breast, lung, pancreas, and oesophagus. It has also been associated with tissue-specific and cell-specific roles in various cancers. It has been shown to modulate several cell-signalling pathways such as EGFR/ERK, NF-κB, p38/MAPK, PI3K/AKT, Wnt/β-catenin, and JAK/STAT along with their targets such as caspases, MMPs, cyclins; tumour suppressor proteins like p53, C/EBPβ, and p-Rb; various cytokines; EMT markers; and many more. Therefore, FXR has high potential as novel biomarkers for the diagnosis, prognosis, and therapy of cancer. Thus, the present review focuses on the diverse role of FXR in different cancers and its agonists and antagonists.
癌症是由于细胞分子改变而引发的致命疾病之一。与癌症相关的其中一种改变是法尼酯X受体（FXR）的差异表达，FXR是一种调节胆汁、胆固醇稳态、脂质和葡萄糖代谢的核受体。已知FXR可调节多种疾病，包括癌症和心血管疾病，这两种疾病是全球报告的导致死亡的主要原因。最近的研究表明，FXR过表达与乳腺癌、肺癌、胰腺癌和食管癌等不同类型癌症的发生和发展有关。它还与各种癌症中的组织特异性和细胞特异性作用相关。已证明它可调节多种细胞信号通路，如EGFR/ERK、NF-κB、p38/MAPK、PI3K/AKT、Wnt/β-连环蛋白和JAK/STAT及其靶标，如半胱天冬酶、基质金属蛋白酶、细胞周期蛋白；肿瘤抑制蛋白，如p53、C/EBPβ和p-Rb；各种细胞因子；上皮-间质转化标志物等等。因此，FXR作为癌症诊断、预后和治疗的新型生物标志物具有很高的潜力。因此，本综述重点关注FXR在不同癌症中的多种作用及其激动剂和拮抗剂。
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