磷酸化
磷酸化级联
核受体
毛皮-1
受体
转录因子
生物
细胞生物学
蛋白质磷酸化
雌激素受体
基因
生物化学
遗传学
蛋白激酶A
癌症
乳腺癌
作者
Sawako Shindo,Satoru Kakizaki,Toshiyuki Sakaki,Yuki Kawasaki,Tsutomu Sakuma,Masahiko Negishi,Ryota Shizu
标识
DOI:10.1016/j.pharmthera.2023.108477
摘要
Nuclear receptors (NR) collectively regulate several biological functions in various organs. While NRs can be characterized by activation of the transcription of their signature genes, they also have other diverse roles. Although most NRs are directly activated by ligand binding, which induces cascades of events leading to gene transcription, some NRs are also phosphorylated. Despite extensive investigations, primarily focusing on unique phosphorylation of amino acid residues in different NRs, the role of phosphorylation in the biological activity of NRs in vivo has not been firmly established. Recent studies on the phosphorylation of conserved phosphorylation motifs within the DNA- and ligand-binding domains confirmed has indicated the physiologically relevance of NR phosphorylation. This review focuses on estrogen and androgen receptors, and highlights the concept of phosphorylation as a drug target.
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