Results 31 to 40 of about 80,501 (258)

Antagonists Selective for Estrogen Receptor α [PDF]

Endocrinology, 2002
To develop compounds that are antagonists on ER(alpha), but not ER(beta), we have added basic side-chains typically found in nonsteroidal antiestrogens to pyrazole compounds that bind with much higher affinity to ER(alpha) than to ER(beta). In this way we have developed basic side-chain pyrazoles (BSC-pyrazoles) that are high affinity, potent ...
Jun, Sun, Ying R, Huang, William R, Harrington, Shubin, Sheng, John A, Katzenellenbogen, Benita S, Katzenellenbogen   +5 more
openaire   +2 more sources

Positive Regulation of Estrogen Receptor Alpha in Breast Tumorigenesis

Cells, 2021
Estrogen receptor alpha (ERα, NR3A1) contributes through its expression in different tissues to a spectrum of physiological processes, including reproductive system development and physiology, bone mass maintenance, as well as cardiovascular and central ...
Lucas Porras, Houssam Ismail, Sylvie Mader   +2 more
doaj   +1 more source

Estradiol-Induced Estrogen Receptor-α Trafficking [PDF]

The Journal of Neuroscience, 2009
Estradiol has rapid actions in the CNS that are mediated by membrane estrogen receptors (ERs) and activate cell signaling pathways through interaction with metabotropic glutamate receptors (mGluRs). Membrane-initiated estradiol signaling increases the free cytoplasmic calcium concentration ([Ca2+]i) that stimulates the synthesis of neuroprogesterone in
Galyna, Bondar, John, Kuo, Naheed, Hamid, Paul, Micevych   +3 more
openaire   +2 more sources

Computer-Aided Ligand Discovery for Estrogen Receptor Alpha [PDF]

International Journal of Molecular Sciences, 2020
Breast cancer (BCa) is one of the most predominantly diagnosed cancers in women. Notably, 70% of BCa diagnoses are Estrogen Receptor α positive (ERα+) making it a critical therapeutic target. With that, the two subtypes of ER, ERα and ERβ, have contrasting effects on BCa cells.
Bafna, Divya, Ban, Fuqiang, Rennie, Paul S., Singh, Kriti, Cherkasov, Artem   +4 more
openaire   +2 more sources

Estrogen alpha receptor antagonists for the treatment of breast cancer: a review

Chemistry Central Journal, 2018
Background Cancer is at present one of the leading causes of death in the world. It accounts for 13% of deaths occurred worldwide and is continuously rising, with an estimated million of deaths up to 2030.
Deepika Sharma, Sanjiv Kumar, Balasubramanian Narasimhan   +2 more
doaj   +1 more source

AIB1/SRC-3/NCOA3 function in estrogen receptor alpha positive breast cancer

Frontiers in Endocrinology, 2023
The estrogen receptor alpha (ERα) is a steroid receptor that is pivotal in the initiation and progression of most breast cancers. ERα regulates gene transcription through recruitment of essential coregulators, including the steroid receptor coactivator ...
Amber J. Kiliti, Amber J. Kiliti, Ghada M. Sharif, Mary Beth Martin, Mary Beth Martin, Anton Wellstein, Anna T. Riegel   +6 more
doaj   +1 more source

Membrane-bound estrogen receptor alpha initiated signaling is dynamin dependent in breast cancer cells

European Journal of Medical Research, 2018
Background Although membrane-associated estrogen receptors (mERs) have been known to play important role in steroid-induced signal transmission, we still know little about their function in the estrogen-induced proliferation of breast cancer cells ...
Istvan Marczell, Petra Balogh, Gabor Nyiro, Anna L. Kiss, Balazs Kovacs, Gabor Bekesi, Karoly Racz, Attila Patocs   +7 more
doaj   +1 more source

VULCAN integrates ChIP-seq with patient-derived co-expression networks to identify GRHL2 as a key co-regulator of ERa at enhancers in breast cancer

Genome Biology, 2019
Background VirtUaL ChIP-seq Analysis through Networks (VULCAN) infers regulatory interactions of transcription factors by overlaying networks generated from publicly available tumor expression data onto ChIP-seq data.
Andrew N. Holding, Federico M. Giorgi, Amanda Donnelly, Amy E. Cullen, Sankari Nagarajan, Luke A. Selth, Florian Markowetz   +6 more
doaj   +1 more source

Definition of the estrogen negative feedback pathway controlling the GnRH pulse generator in female mice

Nature Communications, 2022
Estrogen secreted by the ovary controls how the brain drives pulsatile reproductive hormone secretion. The authors show that in mice, estrogen receptor alpha within a specific population of hypothalamic kisspeptin neurons is the principal pathway through
H. James McQuillan, Jenny Clarkson, Alexia Kauff, Su Young Han, Siew Hoong Yip, Isaiah Cheong, Robert Porteous, Alison K. Heather, Allan E. Herbison   +8 more
doaj   +1 more source

aP2-Cre-mediated inactivation of estrogen receptor alpha causes hydrometra.

PLoS ONE, 2014
In this study we describe the reproductive phenotypes of a novel mouse model in which Cre-mediated deletion of ERα is regulated by the aP2 (fatty acid binding protein 4) promoter.
Per Antonson, Marko Matic, Neil Portwood, Raoul V Kuiper, Galyna Bryzgalova, Hui Gao, Sara H Windahl, Patricia Humire, Claes Ohlsson, Per-Olof Berggren, Jan-Åke Gustafsson, Karin Dahlman-Wright   +11 more
doaj   +1 more source