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Estrogen receptor α (ERα) is a member of the nuclear receptor superfamily of transcription factors encoded by ESR1 in humans that has a key role in reproductive function and additional roles in cancer progression and inhibition.1,2,3 Alternative splicing of the ESR1 pre-mRNA produces one full-length 66 kDa isoform and two short-length 46 and 36 kDa isoforms, which contain truncated C-termini.3 ERα is comprised of an N-terminal domain that contains AF-1, which is critical for the transactivation function of ERα, a DNA-binding domain that recognizes estrogen response elements (EREs) on target genes, and a C-terminal ligand-binding domain (LBD) that contains the nuclear localization signal.2,1 ERα is widely expressed in numerous tissues, including breast, prostate, uterus, liver, and bone, and localizes to the cytoplasm in a complex with heat shock protein 90 (Hsp90).3,2 Upon estrogen stimulation, ERα dissociates from Hsp90, dimerizes, and translocates to the nucleus, where it binds EREs expressed by target genes encoding proteins that activate numerous signaling pathways, including ERK/MAPK, PI3K/Akt/mTOR, and NF-κB, and influence a variety of cellular processes, including reproductive function, bone homeostasis, and inflammation, as well as tumor progression and metastasis.2,1 ERα is overexpressed in more than 50% of patients with breast cancer, but is associated with improved prognosis, whereas loss of ERα is a feature of triple-negative breast cancer (TNBC) and is associated with resistance to hormonal therapy.4 Cayman’s Estrogen Receptor α Rabbit Monoclonal Antibody (Clone RM292) can be used for immunohistochemistry (IHC) and Western blot (WB) applications.
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1. ERα, a key target for cancer therapy: A review. Onco. Targets Ther. 13, 2183-2191 (2020).
2. Membrane and nuclear estrogen receptor alpha actions: From tissue specificity to medical implications. Physiol. Rev. 97(3), 1045-1087 (2017).
3. Mechanisms for estrogen receptor expression in human cancer. Exp. Hematol. Oncol. 7, 24 (2018).
4. Estrogen receptor alpha in human breast cancer: occurrence and significance. J. Mammary Gland Biol. Neoplasia 5(3), 271-281 (2000).