scholarly journals Mechanistic Aspects of Estrogen Receptor Activation Probed with Constitutively Active Estrogen Receptors: Correlations with DNA and Coregulator Interactions and Receptor Conformational Changes

1997 ◽  
Vol 11 (9) ◽  
pp. 1375-1386 ◽  
Author(s):  
Gwendal Lazennec ◽  
Tracy R. Ediger ◽  
Larry N. Petz ◽  
Ann M. Nardulli ◽  
Benita S. Katzenellenbogen
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptors ◽  
Conformational Changes ◽  
Receptor Activation ◽  
Constitutively Active

Binding of Phytoestrogens to Rat Uterine Estrogen Receptors and Human Sex Hormone-binding Globulins

2005 ◽  
Vol 60 (7-8) ◽  
pp. 649-656 ◽  
Author(s):  
Pablo Ibieta Hillerns ◽  
Yuangang Zu ◽  
Michael Wink
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptors ◽  
Conformational Changes ◽  
Nordihydroguaiaretic Acid ◽  
Sex Hormone ◽  
Sex Hormone Binding Globulin ◽  
Scatchard Analysis ◽  
Binding Affinities ◽  
Hormone Binding ◽  
17Β Estradiol

The interaction of phytoestrogens with the most important binding sites of steroid hormones, i.e. sex hormone-binding globulin and estrogen receptors, was investigated. Relative binding affinities and association constants for 21 compounds among them isoflavones, flavones, flavonols, flavanones, chalcones and lignans were determined. The lignan nordihydroguaiaretic acid weakly displaced 17β-[3H]-estradiol from estrogen receptor and Scatchard analysis suggests non-conformational changes. Compounds from Glycyrrhiza glabra, liquiritigenin and isoliquiritigenin, showed estrogenic affinities to both receptors. 18β-Glycyrrhetinic acid displaced 17β-[3H]-estradiol from sex hormone-binding globulin but not from the estrogen receptor. Phytoestrogens compete with 17β-estradiol much stronger than with 5α-dihydrotestosterone for binding to sex hormone-binding globulin.

scholarly journals Hormone and antihormone induce distinct conformational changes which are central to steroid receptor activation.

1992 ◽  
Vol 267 (27) ◽  
pp. 19513-19520 ◽  
Author(s):  
G.F. Allan ◽  
X Leng ◽  
S.Y. Tsai ◽  
N.L. Weigel ◽  
D.P. Edwards ◽  
...  
Keyword(s):  
Conformational Changes ◽  
Steroid Receptor ◽  
Receptor Activation

scholarly journals G Protein-Coupled Estrogen Receptor 1 (GPER) as a Novel Target for Schizophrenia Drug Treatment

2020 ◽  
Vol 1 (1) ◽  
Author(s):  
Danielle S Macêdo ◽  
Lia Lira Olivier Sanders ◽  
Raimunda das Candeias ◽  
Cyntia de Freitas Montenegro ◽  
David Freitas de Lucena ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptors ◽  
G Protein ◽  
Brain Inflammation ◽  
Antipsychotic Treatment ◽  
New Class ◽  
Estrogen Receptor Modulators ◽  
Novel Target ◽  
G Protein Coupled ◽  
Estrogen Receptor 1

Abstract The observation that a person’s sex influences the onset age of schizophrenia, the course of the disease, and antipsychotic treatment response suggests a possible role for estrogen receptors in the pathophysiology of schizophrenia. Indeed, treatment with adjunctive estrogen or selective estrogen receptor modulators (SERMs) are known to reduce schizophrenia symptoms. While estrogen receptors (ER)α and ERβ have been studied, a third and more recently discovered estrogen receptor, the G protein-coupled estrogen receptor 1 (GPER), has been largely neglected. GPER is a membrane receptor that regulates non-genomic estrogen functions, such as the modulation of emotion and inflammatory response. This review discusses the possible role of GPER in brain impairments seen in schizophrenia and in its potential as a therapeutic target. We conducted a comprehensive literature search in the PubMed/MEDLINE database, using the following search terms: “Schizophrenia,” “Psychosis,” “GPER1 protein,” “Estrogen receptors,” “SERMS,” “GPER1 agonism, “Behavioral symptoms,” “Brain Inflammation.” Studies involving GPER in schizophrenia, whether preclinical or human studies, have been scarce, but the results are encouraging. Agonism of the GPER receptor could prove to be an essential mechanism of action for a new class of “anti-schizophrenia” drugs.

Characterization of rodent constitutively active estrogen receptor α variants and their constitutive transactivation mechanisms

2017 ◽  
Vol 248 ◽  
pp. 16-26 ◽  
Author(s):  
Hirotaka Ishii ◽  
Yujiro Hattori ◽  
Arisa Munetomo ◽  
Hiroshi Watanabe ◽  
Yasuo Sakuma ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptor Α ◽  
Constitutively Active

scholarly journals Estrogen receptor (ER) modulators each induce distinct conformational changes in ER   and ER  

1999 ◽  
Vol 96 (7) ◽  
pp. 3999-4004 ◽  
Author(s):  
L. A. Paige ◽  
D. J. Christensen ◽  
H. Gron ◽  
J. D. Norris ◽  
E. B. Gottlin ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Conformational Changes

Expression pattern of estrogen receptors α and β and G-protein-coupled estrogen receptor 1 in the human testis

2014 ◽  
Vol 142 (4) ◽  
pp. 421-432 ◽  
Author(s):  
Daniela Fietz ◽  
Clara Ratzenböck ◽  
Katja Hartmann ◽  
Oksana Raabe ◽  
Sabine Kliesch ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptors ◽  
G Protein ◽  
Expression Pattern ◽  
Human Testis ◽  
G Protein Coupled ◽  
Estrogen Receptor 1
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