Rossini G P, Malaguti C
Dipartimento di Scienze Biomediche, Università di Modena, Italy.
FEBS Lett. 1995 Dec 4;376(3):151-4. doi: 10.1016/0014-5793(95)01264-6.
When MCF-7 cells were treated with 17 beta-estradiol, dexamethasone, or promegestone at 37 degrees C, the KD of receptors for their cognate ligands was found to decrease as compared to that measured at 2 degrees C. Cell incubation with hormone at 37 degrees C did not affect the Bmax of glucocorticoid and progesterone receptors, but caused a 40% increase of that of estrogen receptor. This increase required the presence of ligand, was insensitive to cycloheximide, and was completed within 10 min of cell incubation at physiological temperature. We conclude that an early step of estrogen action is the recruitment of pre-existing receptor molecules through activation of their binding capacity.
当MCF-7细胞在37℃下用17β-雌二醇、地塞米松或炔诺孕酮处理时,发现其同源配体受体的解离常数(KD)与在2℃下测得的相比有所降低。细胞在37℃下与激素孵育不影响糖皮质激素和孕激素受体的最大结合容量(Bmax),但使雌激素受体的Bmax增加了40%。这种增加需要配体的存在,对放线菌酮不敏感,并且在生理温度下细胞孵育10分钟内即可完成。我们得出结论,雌激素作用的早期步骤是通过激活其结合能力来募集预先存在的受体分子。