Steroid hormones receptors (SHRs) are intracellular transcription factors that can be activated by binding specific ligands (i.e., steroid hormones (SH)) to the ligand-binding domain (LBD) (Ray DW et AL. 1999; Pike AC et al. 1999; Bledsoe RK et al. 2002; Li Y et al. 2005; Kumar R and McEwan IJ 2012; Kumar R et al. 2011; Williams SP & Sigler PB 1998; Tanenbaum DM et al. 1998; Lusher SJ et al. 2012). LBD (E-region) resides in the C-terminal half of the receptor and in addition to ligand binding function contains a transcriptional activation function (AF2), sequences for dimerization, heat shock protein association, intermolecular silencing and intramolecular repression (Kumar R and McEwan IJ 2012). The binding of hormone acts as an allosteric switch to regulate SHR-DNA and SHR-protein interactions, including interdomain interactions and/or dimerization (Kumar R and McEwan IJ 2012).
SHS由胆固醇中的肾上腺皮质(糖皮质激素,Mineralocorcoids和肾上腺雄激素)合成,睾丸(睾丸和雌激素,雌激素)和卵巢和胎儿(雌激素和孕激素或孕激素)(Payne Ah和Hales DB 2004; HU J等等。2010;)。SHS通过血液到达靶细胞,它们与特定载体蛋白结合(Grishkovskaya I等,2000; Hammond GL 2016)。SHS从载体蛋白脱离,因为它们的亲脂性本质可以通过细胞的质膜易扩散(oren i等,2004)。在靶细胞内,SHS与类固醇激素受体(SHR)结合,其存在于与热休克蛋白HSP90和共伴侣(例如,Immunophilins P23)中存在于杂蛋白中(例如,Immunophilins P23)(Echeverria PC和Picard D 2010)。HSP90和伴侣介导的构象变化的ATP键合形式的组合变化需要在配体结合主管状态(MCLaughlin Sh等人,2002; Pratt WB等,2008; Krukenberg Ka等,2011)。