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Estrogen receptor transcription and transactivation Estrogen receptor alpha and estrogen receptor beta: regulation by selective estrogen receptor modulators and importance in breast cancer [PDF]
Estrogens display intriguing tissue-selective action that is of great biomedical importance in the development of optimal therapeutics for the prevention and treatment of breast cancer, for menopausal hormone replacement, and for fertility regulation. Certain compounds that act through the estrogen receptor (ER), now referred to as selective estrogen ...
S Katzenellenbogen, Benita +1 more
openaire +2 more sources
In Silico Evaluation of Alpha Mangostin and its Derivatives as a potential Anti-Cancer Agents [PDF]
Alpha-Mangostin, a natural xanthone from Garcinia mangostana, and its structurally optimized derivatives were evaluated as anticancer agents targeting estrogen receptor proteins linked to breast cancer: Estrogen Receptor Alpha(3ERT), Estrogen Receptor ...
V Harini Rakshitha +3 more
doaj +1 more source
Antagonists Selective for Estrogen Receptor α [PDF]
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 +5 more
openaire +2 more sources
Estradiol-Induced Estrogen Receptor-α Trafficking [PDF]
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 +3 more
openaire +2 more sources
Computer-Aided Ligand Discovery for Estrogen Receptor Alpha [PDF]
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 +4 more
openaire +2 more sources
Estrogen alpha receptor antagonists for the treatment of breast cancer: a review
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 +2 more
doaj +1 more source
Positive Regulation of Estrogen Receptor Alpha in Breast Tumorigenesis
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 +2 more
doaj +1 more source
Hypoxia, which is intimately associated with the biology of breast carcinomas, modulates the level of estrogen receptor (ER) alpha expression and transactivation. We investigated the effect of blocking ER degradation on ERalpha-mediated transactivation under hypoxic conditions using the proteasome inhibitor MG132.
Yeo Myeong Park +3 more
openalex +4 more sources
AIB1/SRC-3/NCOA3 function in estrogen receptor alpha positive breast cancer
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 +6 more
doaj +1 more source
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 +7 more
doaj +1 more source

