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选择性雌激素受体调节剂(selective estrogen receptor modulator,SERM)是一类结构多样的化合物,能在不同组织发挥不同的雌激素激动或拮抗作用。其选择性作用机制与自身分子结构、雌激素受体、共调节蛋白以及非基因效应等多方面因素有关,目前仍未完全明确。因雷洛昔芬在骨和心血管组织中表现为雌激素激动作用,在子宫和乳腺组织表现为雌激素拮抗作用,受到了关注,而它在脑、前列腺等组织中的作用尚待研究。现对SERMs的选择性作用机制,以及在骨、子宫、乳腺、心血管、脑、前列腺组织的选择性作用做一综述,重点介绍雷洛昔芬。
Selective estrogen receptor modulators (SERMs) are a diverse class of compounds that exert different estrogenic agonist or antagonistic effects in different tissues. Its selective mechanism of action and its own molecular structure, estrogen receptors, co-regulatory proteins and non-gene effects and many other factors, is still not yet fully clear. Since raloxifene shows estrogen agonism in bone and cardiovascular tissue, estrogen antagonism has been observed in uterine and breast tissues, and its role in brain and prostate tissues remains to be studied. The mechanisms of selective action of SERMs and their selective roles in bone, uterus, breast, cardiovascular, brain, and prostate tissues are now reviewed, highlighting raloxifene.