San Diego Anti-aging medicine and family practice located in Encinitas CA, Center for Age Management

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Center for Age Management

317 N. El Camino Real, Suite 206
Encinitas, CA 92024
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Phone: 760-633-1315

 

Mon - Thur: 9am to 5pm
Lunch: 12pm to 1:30pm
Friday: 9am to 12pm
On Fridays, we will have limited staff. You may leave a message and it will be our pleasure to return your call. Any prescriptions, questions or concerns that you have, we will be happy to assist you Monday - Thursday.

Serving other neighboring cities: La Costa, Solana Beach, Rancho Santa Fe, Del Mar, San Marcos, Carlsbad, La Jolla, and San Diego County, CA.

Estriol acts as a GPR30 antagonist in estrogen receptor-negative breast cancer cells

Mol Cell Endocrinol. 2010 May 14;320(1-2):162-70. Epub 2010 Feb 6.
Lappano R, Rosano C, De Marco P, De Francesco EM, Pezzi V, Maggiolini M.
Dipartimento Farmaco-Biologico, Università della Calabria, Rende (CS), Italy.

Abstract

Estrogens are structurally related steroids that regulate important physiological processes. 17beta-estradiol (E2) is reversibly oxidized to estrone (E1) and both E2 and E1 can be irreversibly converted to estriol (E3), which also originates directly from androstenedione. The action of E2 has been traditionally explained by the binding to the estrogen receptor (ER) alpha and ER beta, however the G protein-coupled receptor (GPR) 30 has been recently involved in the rapid signaling triggered by estrogens. Although the role of E2 in the development of breast cancer has been largely documented, the contribution of E3 still remains to be completely evaluated. Here, we demonstrate for the first time that E3 acts as a GPR30 antagonist since it was able to inhibit the GPR30-mediated responses such as the rapid ERK activation, the up-regulation of target genes like c-fos and connective tissue growth factor, the proliferative effects observed in ER-negative SkBr3 cells. (c) 2010 Elsevier Ireland Ltd. All rights reserved.

PMID: 20138962 [PubMed – indexed for MEDLINE]