TY - JOUR
T1 - 27-Hydroxycholesterol, an endogenous selective estrogen receptor modulator
AU - He, Sisi
AU - Nelson, Erik R.
N1 - Funding Information:
This work was supported by the National Institutes of Health under award number R00CA172357 (E.R.N.) and a Cancer Scholars for Translational and Applied Research (C*STAR) Award (S.H.). The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health or the Carle Foundation Hospital.
PY - 2017/10
Y1 - 2017/10
N2 - 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.
AB - 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.
KW - 27-hydroxycholesterol
KW - Cholesterol
KW - Estrogen
KW - Estrogen receptor
KW - Selective estrogen receptor modulator
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U2 - 10.1016/j.maturitas.2017.07.014
DO - 10.1016/j.maturitas.2017.07.014
M3 - Review article
C2 - 28923174
AN - SCOPUS:85027247881
VL - 104
SP - 29
EP - 35
JO - Maturitas
JF - Maturitas
SN - 0378-5122
ER -