Bisphenol A induces a rapid activation of Erk1/2 through GPR30 in human breast cancer cells

International Union of Basic and Clinical Pharmacology. XCVII. G Protein–Coupled Estrogen Receptor and Its Pharmacologic Modulators

“…In cell lines of thyroid, ovarian, endometrial, and breast cancers, stimulation of GPER with E2 (Vivacqua et al, 2006a,b;Albanito et al, 2007) or other estrogenic compounds, such as genistein (Vivacqua et al, 2006a), bisphenol A (Dong et al, 2011;Chevalier et al, 2012a), or tamoxifen (Vivacqua et al, 2006b) activates signaling mechanisms that typically promote proliferation. Furthermore, in endometrial (Smith et al, 2007) and ovarian cancer (Smith et al, 2009), high GPER expression correlated with poor survival, although a recent study reported the opposite in ovarian cancer (Ignatov et al, 2013a).…”

Estrogen-responsive genes for environmental studies

“…While BPA has been known to bind to both ERα and ERβ [85], it induces the rapid activation of ERK1 and ERK2 (ERK1/2) even in ERα/β-negative breast cancer cells (Fig. 2D; [86]). This effect is not blocked by ER antagonists, and the expression of GPR30 is necessary for BPA-induced activation of ERK1/2 and the transcriptional regulation of c-fos (FOS).…”

“…Alternatively, appropriate standardization would be needed to compare data from different DNA microarray platforms or protocols and to solve many of the problems of microarray data, especially when they are used for humans, such as a risk assessment of endocrine disruptors. [77]), zearalenone (panel C; [83]), bisphenol A (panel D; [86]) and estrogen in the rat brain (panel E; [100]). The genes (proteins) related to but not listed as estrogen-responsive genes identified are parenthesized in panel A.…”

Protective Effect of 3, 3-Diindolylmethane on Bisphenol A Activated GPR30, RAS, PI3K/Akt Estrogenic Signaling Pathway in Female Sprague-Dawley Rats

“…The recent study reported that BPA-induced cell proliferation occurs via JAK/Stat3, MAPK/ERK and PI3K/Akt pathways [25]. BPA can exert Erk1/2/c-fos signaling through GPR30 in SKBR3 cells and up-regulate the expression of an AP1-target gene pS2 via a pathway induced by Erk1/2/c-fos signaling [26]. In this study, western blot analysis showing over expression of GPR30, SRC, Ras, PI3K and Akt and immunohistochemical analysis shows increased expression of PCNA in mammary glands of BPA alone treated rats.…”