选择性雌激素受体调节剂组织选择性作用研究进展

Research progress on tissue selectivity of selective estrogen receptor modulators

选择性雌激素受体调节剂(SERMs)是作用在雌激素受体上,在不同的靶组织细胞中起激动剂或拮抗剂调节作用的药物。SERMs本身结构特异性及其与不同靶组织中的受体形成复合体的差异决定了其在各类组织选择性的不同。综述了目前临床常见SERMs的结构类型及其在乳腺、骨、心血管、子宫、肝脏、神经等组织选择性作用的研究进展;并且跟踪报道了治疗绝经期综合症及预防绝经后骨质疏松症的一个新方式即由SERMs与雌激素形成的组织选择性雌激素复合物的应用状况。

Selective estrogen receptor modulators （SERMs） can exhibit estrogen receptors （ERs） agonist or antagonist activity depending on the cell target tissue. The selective differences of SERMs are determined by the structure specificity of SERMs and diversity of the receptor-ligand complex in various target tissue. The structures of usual clinic SERMs and the SERMs＇ tissue selectivity effects in mammary gland, bone, cardiovascular, endometrial, liver and nervus tissue are reviewed in this paper, what＇s more, a newer promising approach to menopausal therapy and prevention of postmenopausal osteoporosis, the tissue selective estrogen complex （TSEC）, pairing a SERM with one or more estrogens with the goal of maintaining the benefits of estrogens without the stimulatory effects on the breast and uterus is reoorted currently in this patper.