THE GOOD, BETTER AND BEST ABOUT SELECTIVE ESTROGEN RECEPTOR MODULATORS AS NOVEL GUARDIANS AGAINST OSTEOPOROSIS

Abstract

The functions of estrogen are highly significant in human physiology. The regulatory effect of estrogen is mediated through three distinct estrogen receptors (ER), namely estrogen receptor alpha (ER α), estrogen receptor beta (ER β) and G protein coupled estrogen receptor (GPCER). Selective estrogen receptor modulators (SERMs) are synthetic/ natural molecules that aid in transcriptional roles such as estrogen agonistic / antagonist activity in target tissues by binding to ER. These compounds lack the steroidal back bone of estrogen but structurally resemble estrogen and hence can compete with estrogen and bind to estrogen responsive elements. This in turn triggers downstream signaling pathways that decide the fate of the cell to transit between proliferation and death. This review article describes the various synthetic and natural SERMS, their chemical classification, mechanism of action, side effects, bioavailability and clinical implications in several pathogenic conditions majorly in osteoporosis. This is based on a systematic review and consideration of the recent literature on various approaches (Pharmacogenomics, nutrigenomics, Pharmaconutritional approaches) on osteoporosis and strategies involved in the management of its clinical symptoms. Osteoporosis is a growing health burden all over the world, affecting the quality of life especially in elderly women population. Apart from the role of SERMs in osteoporosis, this review summarizes the promising roles of SERMs in other pathologic conditions like breast cancer, cardiovascular diseases, neuroprotection and reproductive biology. Hence the exploitation of SERMs as therapeutic and prophylactic agents with increased tolerability, safety and efficacy is an area of booming research in the recent decades.