27-Hydroxycholesterol, an endogenous selective estrogen receptor modulator.
Estrogen receptors (ERs) mediate the actions of the steroidal estrogens, and are important for the regulation of several physiological and pathophysiological processes, including reproduction, bone physiology, cardiovascular physiology and breast cancer. The unique pharmacology of the ERs allows for certain ligands, such as tamoxifen, to elicit tissue- and context-specific responses, ligands now referred to as selective estrogen receptor modulators (SERMs). Recently, the cholesterol metabolite 27-hydroxychoelsterol (27HC) has been defined as an endogenous SERM, with activities in atherosclerosis, osteoporosis, breast and prostate cancers, and neural degenerative diseases. Since 27HC concentrations closely mirror those of cholesterol, it is possible that 27HC mediates many of the biological effects of cholesterol. This paper provides an overview of ER pharmacology and summarizes the work to date implicating 27HC in various diseases. Wherever possible, we highlight clinical data in support of a role for 27HC in the diseases discussed.
['He|Sisi|S|', 'Nelson|Erik R|ER|']
D000818:Animals D050197:Atherosclerosis D001943:Breast Neoplasms D060825:Cognitive Dysfunction D005260:Female D006801:Humans D006888:Hydroxycholesterols D008297:Male D010024:Osteoporosis D011471:Prostatic Neoplasms D011960:Receptors, Estrogen D020845:Selective Estrogen Receptor Modulators
27-hydroxycholesterol Selective estrogen receptor modulator Estrogen Estrogen receptor Cholesterol