[關(guān)鍵詞]
[摘要]
選擇性雌激素受體調(diào)節(jié)劑(SERMs)是作用在雌激素受體上,在不同的靶組織細(xì)胞中起激動(dòng)劑或拮抗劑調(diào)節(jié)作用的藥物。SERMs本身結(jié)構(gòu)特異性及其與不同靶組織中的受體形成復(fù)合體的差異決定了其在各類組織選擇性的不同。綜述了目前臨床常見SERMs的結(jié)構(gòu)類型及其在乳腺、骨、心血管、子宮、肝臟、神經(jīng)等組織選擇性作用的研究進(jìn)展;并且跟蹤報(bào)道了治療絕經(jīng)期綜合癥及預(yù)防絕經(jīng)后骨質(zhì)疏松癥的一個(gè)新方式即由SERMs與雌激素形成的組織選擇性雌激素復(fù)合物的應(yīng)用狀況。
[Key word]
[Abstract]
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 reported currently in this paper.
[中圖分類號(hào)]
[基金項(xiàng)目]