Estrogen Receptor β in the Pharmacology of Estrogens and Antiestrogens

Autor: G. Kuiper, M. Warner, J.-Å Gustafsson
Rok vydání: 1999
Předmět:
Zdroj: Handbook of Experimental Pharmacology ISBN: 9783642642616
Popis: The discovery of the second type of estrogen receptor (ER), ER β (KUIPER et al. 1996), changed the way we understand the physiological and pharmacological actions of estrogens and anti estrogens. The findings of multiple isoforms of ER ,β (CHU and FULLER 1997; TREMBLAY et al. 1997; MARUYAMA et al. 1998; MOORE et al. 1998; OGAWA et al. 1998a,b; PETERSEN et al. 1998) and multiple sites on DNA where these receptors can act (WEBB et al. 1995; YANG et al. 1996; PAECH et al. 1997; PORTER et al. 1997; UHT et al. 1997; MONTANO et al. 1998) introduce levels of complexity to the mechanisms of estrogen action that were previously unimagined. Many aspects of the actions of estrogens and antiestrogens have mystified pharmacologists for a long time (KATZENELLENBOGEN et al. 1996). It was very difficult to understand how estradiol could increase the risk of breast cancer, whereas phytoestrogens would reduce it, if they were acting on only one type of ER (INGRAM et al. 1997; STEPHENS 1997; HILAKIVI-CLARKE et al. 1998). Equally puzzling were the differential tissue effects of the antiestrogen tamoxifen, which is an estrogen antagonist in the breast but an agonist in the uterus, cardiovascular system and bone (BRYANT and DERE 1998).
Databáze: OpenAIRE