Lin M T, Rao C V
Mol Cell Endocrinol. 1978 Jan;9(3):311-20. doi: 10.1016/0303-7207(78)90073-4.
Selected properties of [3H]prostaglandin (PG) E1 binding to collagenase dispersed bovine luteal cells were studied and compared with those observed in luteal plasma membranes. [3H]-PGE1 specific binding to a relatively homogeneous population of luteal cells was a rapid (K1 = 4.2 X 10(5) M-1 .sec-1), reversible (K-1 = 3.9 X 10(-3) sec-1), saturable and specific process at 38 degrees C. The binding was homogeneous with an apparent dissociation constant of 2.4 nM and 1.8 X 10(5) receptors per cell. The presence of increasing amounts of unlabeled PGs inhibited [3H]PGE1 binding in a dose-dependent manner. The potency order for this inhibition of binding was: PGE 2 greater than PGE1, (15S)-15-methyl-PGE2 methyl ester greater than PGF2alpha greater than PGF1alpha greater than other PGs, PGE, PGF metabolites and PGF analogs. Other than the homogeneous nature of [3H]PGE1 binding and the greater effectiveness of PGE2 compared to PGE1 in cells, the rest of the properties of [3H]PGE1 binding to cells were in excellent agreement with those observed in plasma membranes.
研究了[3H]前列腺素(PG)E1与胶原酶分散的牛黄体细胞结合的特定性质,并与在黄体细胞膜中观察到的性质进行了比较。[3H]-PGE1与相对同质的黄体细胞群体的特异性结合在38℃下是一个快速(K1 = 4.2×10(5) M-1·sec-1)、可逆(K-1 = 3.9×10(-3) sec-1)、可饱和且特异的过程。结合是同质的,表观解离常数为2.4 nM,每个细胞有1.8×10(5)个受体。未标记PGs量的增加以剂量依赖性方式抑制[3H]PGE1结合。这种结合抑制的效力顺序为:PGE2大于PGE1,(15S)-15-甲基-PGE2甲酯大于PGF2α大于PGF1α大于其他PGs、PGE、PGF代谢物和PGF类似物。除了[3H]PGE1结合的同质性以及PGE2在细胞中比PGE1更有效外,[3H]PGE1与细胞结合的其余性质与在细胞膜中观察到的性质非常一致。