Effects of fulvestrant, an estrogen receptor antagonist, on MMQ cells and its mechanism.
OBJECTIVES: Unlike the successful endocrine therapy of breast cancers and other estrogen-dependent diseases, little is known about the effect of anti-estrogen treatment on pituitary tumors. Our objectives were to study the effect of fulvestrant, a new type anti-estrogen devoid of any agonistic activities, on prolactinoma cell line MMQ in vitro and its possible mechanisms.
DESIGN: In the experiment, the prolactin concentration, proliferation and apoptosis of the MMQ cell were measured to investigate the anti-tumor effect of the fulvestrant. The expression of estrogen receptor (ESR) mRNA and protein and MAPK pathway-related proteins ERK1 and 2, JNK, and p38 were measured to investigate the possible mechanisms.
RESULTS: Fulvestrant significantly inhibited prolactin secretion (up to 85.5%), decreased proliferation (IC50 = 32.4 nmol/l), and promoted apoptosis of the MMQ cells.
CONCLUSIONS: The suppression was possibly mediated by inhibition of ESR mRNA expression, down-regulation of ESR expression and activation of MAPK pathway-related proteins. Thus, fulvestrant has suppressive effects on prolactinoma cells and its anti-tumor mechanism appears to be related to the inhibition of ESR and the MAPK pathway....
Citation
Li C, Sun Z, Gui S, Liu F, Zhang Y. Effects of fulvestrant, an estrogen receptor antagonist, on MMQ cells and its mechanism. Neuro Endocrinol Lett. 2009 Jan; 30(2): 268-274