Elucidation of the molecular mechanism of action of selective estrogen receptor modulators
Elucidation of the molecular mechanism of action of selective estrogen receptor modulators
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DOI：
10.1016/s0002-9149(01)02221-4
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发表时间：
2002-07-03
影响因子：
2.8
通讯作者：
Norris, JD
中科院分区：
文献类型：
--
作者：
McDonnell, DP;Wijayaratne, A;Norris, JD
术语选择性雌激素受体调节剂（SERM）描述了一组在某些组织中表现出雌激素受体（ER）激动剂活性，但在其他组织中反对雌激素作用的药物。虽然描述这类药物的名称是新的，但概念不是，因为表现出组织选择性ER激动剂/拮抗剂特性的化合物已经存在了近40年。什么是新的想法，它可能是利用的矛盾活动的SERM和开发它们作为目标器官选择性ER激动剂治疗骨质疏松症和其他雌激素。这一认识为这一领域的研究提供了动力，本文综述了这一领域的研究进展。(C)2002年，Excerpta Medica，Inc.
The term selective estrogen receptor modulator (SERM) describes a group of pharmaceuticals that manifest estrogen receptor (ER) agonist activity in some tissues,but opposes estrogen action in others. Although the name describing this class of drugs is new, the concept is not, as compounds exhibiting tissue-selective ER agonist/antagonist properties have been available for nearly 40 years. What is new is the idea that it may be possible to capitalize on the paradoxical activities of SERMs and develop them as target organ-selective ER agonists for the treatment of osteoporosis and other estrogenopathies. This realization has provided the impetus for research in this area, the progress of which is described in this review. (C) 2002 by Excerpta Medica, Inc.