Vallette G, Benassayag C, Christeff N, Clerc F, Nunez E A
Dev Pharmacol Ther. 1984;7 Suppl 1:30-7.
We studied the effects of different classes of non-esterified fatty acids (NEFA) on the binding of natural and synthetic estrogens by uterine cytosolic receptors. The role of alpha 1-fetoprotein (AFP) in this process was also studied. Saturated fatty acids, irrespective of their concentration, slightly increased (120%) E2 binding to the 4S and 8S uterine cytosolic receptors. The effect of unsaturated fatty acids was dependent on their concentration: at 0.5 X 10(-4) M unsaturated NEFA potentiated the E2 binding to the receptor. At a higher concentration (2.0 X 10(-4) M), the NEFAs were highly inhibitory. This inhibition was dependent on the degree of unsaturation of the fatty acids. Tritiated arachidonic acid interacted directly with the 4S and 8S cytosol receptor. Furthermore, we demonstrated a double competition between murine AFP and the 8S receptor for estrogens and unsaturated NEFA. The effect of these hydrophobic ligand exchanges between transport proteins and receptors on the modulation of the action of estrogen is discussed.
我们研究了不同种类的非酯化脂肪酸(NEFA)对子宫胞质受体结合天然和合成雌激素的影响。同时也研究了α1-甲胎蛋白(AFP)在此过程中的作用。饱和脂肪酸,无论其浓度如何,都会使E2与4S和8S子宫胞质受体的结合略有增加(120%)。不饱和脂肪酸的作用取决于其浓度:在0.5×10⁻⁴ M时,不饱和NEFA增强了E2与受体的结合。在较高浓度(2.0×10⁻⁴ M)时,NEFA具有高度抑制作用。这种抑制作用取决于脂肪酸的不饱和程度。氚标记的花生四烯酸直接与4S和8S胞质受体相互作用。此外,我们证明了小鼠AFP与8S受体在雌激素和不饱和NEFA方面存在双重竞争。讨论了这些转运蛋白和受体之间疏水配体交换对雌激素作用调节的影响。