Estrogen receptor alpha (Mouse) (ESR1)

Estrogen receptor alpha (ESR1) is a ligand-activated transcription factor and a member of the nuclear hormone receptor superfamily that mediates the physiological effects of estrogens [UniProt: P19785]. In mice, the Esr1 gene is essential for the development and function of the female reproductive system, as well as for maintaining bone density and regulating metabolic homeostasis [NCBI Gene: 13982]. Upon binding to ligands like 17β-estradiol, the receptor dimerizes and binds to estrogen response elements in the DNA to modulate the transcription of target genes involved in cell growth and differentiation [PubMed: 29111918]. ESR1 is a primary driver in the majority of breast cancers, where its signaling pathway is exploited to promote tumor progression [PubMed: 30215131]. Therapeutic intervention typically involves the use of selective estrogen receptor modulators (SERMs) or degraders (SERDs) to inhibit its activity [PubMed: 28211447]. While the protein is the traditional drug target, the Esr1 mRNA itself is increasingly investigated as a target for antisense oligonucleotides and RNA interference to overcome resistance to endocrine therapies by preventing receptor synthesis [PubMed: 25611381].

Other names

ER-alphaNR3A1Estradiol receptorNuclear receptor subfamily 3 group A member 1EsrEreEsr1Esr1 mRNA

Selective estrogen receptor modulation (SERM), Selective estrogen receptor degradation (SERD), Competitive antagonism, Agonism, and Antisense inhibition of mRNA translation