Department of Cell Biology, Physiology and Immunology, School of Biology, University of Barcelona, Barcelona, 08028, Spain; Institute of Biomedicine of the University of Barcelona (IBUB), Barcelona, 08028, Spain.
Institute of Biomedicine of the University of Barcelona (IBUB), Barcelona, 08028, Spain; Department of Biochemistry and Molecular Biomedicine, School of Biology, University of Barcelona, Barcelona, 08028, Spain.
Semin Cancer Biol. 2021 Aug;73:58-75. doi: 10.1016/j.semcancer.2020.12.007. Epub 2020 Dec 9.
Nuclear receptors (NRs) are a superfamily of ligand-activated transcription factors that act as biological sensors and use a combination of mechanisms to modulate positively and negatively gene expression in a spatial and temporal manner. The highly orchestrated biological actions of several NRs influence the proliferation, differentiation, and apoptosis of many different cell types. Synthetic ligands for several NRs have been the focus of extensive drug discovery efforts for cancer intervention. This review summarizes the roles in tumour growth and metastasis of several relevant NR family members, namely androgen receptor (AR), estrogen receptor (ER), glucocorticoid receptor (GR), thyroid hormone receptor (TR), retinoic acid receptors (RARs), retinoid X receptors (RXRs), peroxisome proliferator-activated receptors (PPARs), and liver X receptors (LXRs). These studies are key to develop improved therapeutic agents based on novel modes of action with reduced side effects and overcoming resistance.
核受体(NRs)是配体激活的转录因子超家族,作为生物传感器,以时空方式调节基因表达的正性和负性,使用多种机制。几种 NR 的高度协调的生物学作用影响许多不同细胞类型的增殖、分化和凋亡。几种 NR 的合成配体一直是癌症干预的广泛药物发现努力的重点。本文综述了几种相关 NR 家族成员(即雄激素受体(AR)、雌激素受体(ER)、糖皮质激素受体(GR)、甲状腺激素受体(TR)、视黄酸受体(RARs)、维甲酸 X 受体(RXRs)、过氧化物酶体增殖物激活受体(PPARs)和肝 X 受体(LXRs))在肿瘤生长和转移中的作用。这些研究是开发基于新作用模式的改进治疗剂的关键,这些治疗剂具有减少副作用和克服耐药性的作用。