It is well known that sex steroids, in particular estrogens, play an important role in longitudinal bone growth during puberty. High doses of estrogen therapy can reduce the final height of an individual, but such treatment is also associated with severe side effects. At the same time, attenuation of estrogen production by aromatase inhibitors increases adult final height, inhibiting bone turno...

Tamoxifen (TAM), a non-steroidal antiestrogen, has revolutionized female breast cancer treatment. The mechanism involves is to compete with 17β-estradiol (E2) at the receptor site and blocking promotional role of E2 in cancer. Tam pioneering medicine because its widespread usage treatment chemoprevention, as well research into novel selective estrogen modulators (SERMs). In vast majority patien...

Breast cancer is one of the extensively diagnosed cancers and dominating reason women’s death globally. Selective estrogen receptor modulators (SERMs) such as Tamoxifen approved by Food Drug Administration (FDA) for therapy of+ breast tumors may cause negative side effects . Hence, there urgent demand more effective drugs to combat this disease. Molecular docking screening in combination with A...

Primary hyperparathyroidism (PHPT) is a common endocrinopathy, frequently caused by a parathyroid adenoma, rarely by a parathyroid carcinoma that lacks effective oncological treatment. As the majority of cases are present in postmenopausal women, oestrogen signalling has been implicated in the tumourigenesis. Oestrogen receptor beta 1 (ERB1) and ERB2 have been recently identified in parathyroid...

OBJECTIVE Selective estrogen receptor modulators (SERMs) inhibit constriction of mammalian conduit arteries. However, it is unknown whether SERMs at therapeutically achievable concentrations could reduce vascular tone in resistance arteries. The present study aimed to examine roles of Ca(2+) influx in endothelium and endothelial nitric oxide synthase (eNOS) activation in dilatations induced by ...

Estrogen has many positive effects on neural tissue in experimental model systems, including stimulation of neurite growth and neurotransmitter synthesis and protection against diverse types of neural injury. In humans, estrogen treatment is reputed to protect against Alzheimer's disease. To investigate potential mediators of estrogen's action and determine whether selective estrogen receptor m...

Estrogenic industrial compounds such as bisphenol A (BPA) and nonylphenol typically bind estrogen receptor (ER) alpha and ERBeta and induce transactivation of estrogen-responsive genes/reporter genes, but their potencies are usually greater than or equal to 1,000-fold lower than observed for 17Beta-estradiol. Risk assessment of estrogenic compounds on the basis of their potencies in simple repo...

Tamoxifen (Tam) is a selective estrogen receptor (ER) modulator (SERM) that is an essential drug to treat ER-positive breast cancer. Aside from known actions at ERs, recent studies have suggested that some SERMs like Tam also exhibit novel activity at cannabinoid subtype 1 and 2 receptors (CB1R and CB2Rs). Interestingly, cis- (E-Tam) and trans- (Z-Tam) isomers of Tam exhibit over a 100-fold dif...

The phenomenon of mutual annihilation of action between 17 estradiol (E2) and a selective estrogen receptor modulator (SERM), previously described in prepubertal rat diaphysis, epiphysis and uterus, has been investigated in ROS 17/2.8 rat osteoblastic cells and in transiently co-transfected cells in culture. In ROS 17/2.8 cells, the estrogen-induced marker enzyme creatine kinase B (CKB) was sti...