2009•Biological and Pharmaceutical BulletinOpen access

Effects of Inhibiting the Proteasomal Degradation of Estrogen Receptor .ALPHA. on Estrogen Receptor .ALPHA. Activation under Hypoxic Conditions

Yeo Myeong Park, Jung Yoon Cho, Young Do Koo, Young Ju Lee

Abstract

Hypoxia, which is intimately associated with the biology of breast carcinomas, modulates the level of estrogen receptor (ER) alpha expression and transactivation. We investigated the effect of blocking ER degradation on ERalpha-mediated transactivation under hypoxic conditions using the proteasome inhibitor MG132. Pretreatment with MG132 blocked hypoxia-induced degradation of ERalpha protein. Our data imply that ERalpha proteasomal inhibition is linked to receptor transactivation under hypoxia.

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Key concepts: MG132, Transactivation, Estrogen receptor, Estrogen receptor alpha, Estrogen, Estrogen receptor beta, Chemistry, Proteasome inhibitor