Department of Biochemistry and Molecular Biology, Third Military Medical University, Chongqing 400038, China.
J Steroid Biochem Mol Biol. 2011 Nov;127(3-5):231-7. doi: 10.1016/j.jsbmb.2011.08.004. Epub 2011 Aug 22.
Estrogen receptors (ERs) belong to the nuclear receptor superfamily, whose members include ER-α66, ER-α36, ER-α46 and ER-β. Each receptor performs specific functions through binding with a specific ligand, such as estrogen. Recently, ER-α36, a novel variant of human estrogen receptor-alpha (ER-α), was identified and cloned. ER-α36 inhibits, in a dominant-negative manner, the transactivation of both the wild-type ER-α (ER-α66) and ER-β. As a predominantly membrane-based ER, ER-α36 mediates nongenomic estrogen signaling and is involved in the resistance of breast cancer to endocrine therapy, i.e., tamoxifen. This review summarizes recent studies on the structure and function of ER-α36 and the relationship of ER-α36 with cancer, with special emphasis on its function in the resistance of breast cancer to endocrine therapy.
雌激素受体（ERs）属于核受体超家族，其成员包括 ER-α66、ER-α36、ER-α46 和 ER-β。每个受体通过与特定配体（如雌激素）结合来执行特定的功能。最近，人类雌激素受体-α（ER-α）的一种新型变体 ER-α36 被鉴定和克隆。ER-α36 以显性负性方式抑制野生型 ER-α（ER-α66）和 ER-β 的转录激活。作为一种主要基于膜的 ER，ER-α36 介导非基因组雌激素信号转导，并参与乳腺癌对内分泌治疗（即他莫昔芬）的耐药性。本文综述了 ER-α36 的结构和功能及其与癌症的关系的最新研究进展，特别强调了其在乳腺癌内分泌治疗耐药中的作用。
