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A Selective Ligand for Estrogen Receptor Proteins Discriminates Rapid and Genomic Signaling

Journal article
Authors C. M. Revankar
C. G. Bologa
R. A. Pepermans
G. Sharma
W. K. Petrie
S. N. Alcon
A. S. Field
C. Ramesh
M. A. Parker
N. P. Savchuk
L. A. Sklar
H. J. Hathaway
J. B. Arterburn
Tudor I Oprea
E. R. Prossnitz
Published in Cell Chemical Biology
Volume 26
Issue 12
Pages 1692-1702.e5
ISSN 2451-9448
Publication year 2019
Published at Institute of Medicine, Department of Rheumatology and Inflammation Research
Pages 1692-1702.e5
Language en
Keywords breast-cancer, international-union, nongenomic actions, gene-expression, gper function, activation, gpr30, alpha, agonists, cells, Biochemistry & Molecular Biology
Subject categories Biochemistry and Molecular Biology


Estrogen exerts extensive and diverse effects throughout the body of women. In addition to the classical nuclear estrogen receptors (ER alpha and ER beta), the G protein-coupled estrogen receptor GPER is an important mediator of estrogen action. Existing ER-targeted therapeutic agents act as GPER agonists. Here, we report the identification of a small molecule, named AB-1, with the previously unidentified activity of high selectivity for binding classical ERs over GPER. AB-1 also possesses a unique functional activity profile as an agonist of transcriptional activity but an antagonist of rapid signaling through ER alpha. Our results define a class of small molecules that discriminate between the classical ERs and GPER, as well as between modes of signaling within the classical ERs. Such an activity profile, if developed into an ER antagonist, could represent an opportunity for the development of first-in-class nuclear hormone receptor-targeted therapeutics for breast cancer exhibiting reduced acquired and de novo resistance.

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