Masonic Cancer Center, University of Minnesota, Minneapolis, Minnesota.
Division of Hematology, Oncology, and Transplantation, Department of Medicine, University of Minnesota, Minneapolis, Minnesota.
Endocrinology. 2018 Dec 1;159(12):3897-3907. doi: 10.1210/en.2018-00831.
Steroid hormone receptors (SRs) have a multitude of functions in human biology and disease progression. The SR family of related ligand-activated transcription factors includes androgen, estrogen, glucocorticoid, mineralocorticoid, and progesterone receptors. Antiestrogen or estrogen receptor (ER)-targeted therapies to block ER action remain the primary treatment of luminal breast cancers. Although this strategy is successful, ∼40% of patients eventually relapse due to endocrine resistance. The majority of hormone-independent tumors retain some level of SR expression, but sidestep hormone ablation treatments. SRs are known to crosstalk extensively with kinase signaling pathways, and this interplay has been shown to bypass ER-targeted therapies in part by providing alternative proliferation and survival signals that enable hormone independence. Modified receptors adopt alternate conformations that resist antagonism or promote agonism. SR-regulated transcription and SR-binding events have been classically studied as single receptor events using single hormones. However, it is becoming increasingly evident that individual steroids and SRs rarely act alone. Emerging evidence shows that coexpressed SRs crosstalk with each other in hormone-driven cancers, such as breast and prostate. Crosstalk between related SRs allows them to modulate signaling and transcriptional responses to noncognate ligands. This flexibility can lead to altered genomic binding and subsequent changes in SR target gene expression. This review will discuss recent mechanistic advances in elucidating SR crosstalk and the implications for treating hormone-driven cancers. Understanding this crosstalk (i.e., both opposing and collaborative) is a critical step toward expanding and modernizing endocrine therapies and will ultimately improve patient outcomes.
甾体激素受体(SRs)在人类生物学和疾病进展中具有多种功能。相关配体激活转录因子的 SR 家族包括雄激素、雌激素、糖皮质激素、盐皮质激素和孕激素受体。抗雌激素或雌激素受体(ER)靶向治疗以阻断 ER 作用仍然是腔型乳腺癌的主要治疗方法。尽管这种策略是成功的,但约 40%的患者最终因内分泌抵抗而复发。大多数激素非依赖性肿瘤仍然保留一定水平的 SR 表达,但回避激素消融治疗。SR 与激酶信号通路广泛相互作用,这种相互作用已被证明部分通过提供替代增殖和存活信号来绕过 ER 靶向治疗,从而使激素依赖性肿瘤失去作用。修饰后的受体采用替代构象,抵抗拮抗剂或促进激动剂。SR 调节的转录和 SR 结合事件一直被经典地研究为使用单个激素的单个受体事件。然而,越来越明显的是,个体类固醇和 SR 很少单独起作用。新出现的证据表明,在激素驱动的癌症(如乳腺癌和前列腺癌)中,共表达的 SR 相互作用。相关 SR 之间的串扰允许它们调节信号和转录反应,以非同源配体。这种灵活性会导致基因组结合的改变,并随后导致 SR 靶基因表达的改变。这篇综述将讨论阐明 SR 串扰的最新机制进展及其对治疗激素驱动的癌症的影响。了解这种串扰(即,对抗和协作)是扩展和现代化内分泌治疗的关键步骤,最终将改善患者的预后。