Rossini G P, Fayard J M, Tessier C, Laugier C
INSERM U. 352, Laboratoire de Physiologie Pharmacodynamie, Villeurbanne, France.
Biochem J. 1996 May 1;315 ( Pt 3)(Pt 3):1007-14. doi: 10.1042/bj3151007.
The cellular uptake of extracellular type-I phospholipase A2 (PLA2) was investigated in rat uterine stromal cells (UIII) in culture, which were found to express the high-affinity binding site for mammalian type-I PLA2, with a measured KD of 6.4 nM, a Bmax of 0.1-1 pmol/mg of DNA at 4 degrees C, and a molecular mass of about 200 kDa. When UIII cells were treated with type-I PLA2 at 37 degrees C, the ligand specifically associated with the cells increased, reaching a plateau after 90 min of incubation, whose level was about 5-fold higher than that measured if cells were maintained at 4 degrees C. We could determine that the PLA2 was bound to plasma membrane receptors which were responsible for internalization of the ligand, and that the binding sites were still suitable for binding at the level of plasma membrane during UIII cell incubation at 37 degrees C. Proteolysis of internalized PLA2 could be clearly detected only after 90 min of UIII cell incubation with the ligand at 37 degrees C, and most of the intracellular PLA2 consisted of the apparently intact 14 kDa enzyme. By cross-linking studies, we found that most of the internalized PLA2 was not associated with the receptor, supporting the conclusion that in our experimental system a single pool of membrane receptors for mammalian type-I PLA2 undergoes cycles of ligand binding, intracellular transfer and release of PLA2, followed by restoration of binding sites on the plasma membrane. We calculated that the rate of internalization of the ligand by one receptor molecule in UIII cells at 37 degrees C is about three molecules of type-I PLA2 per h.
在培养的大鼠子宫基质细胞(UIII)中研究了细胞对细胞外I型磷脂酶A2(PLA2)的摄取。发现这些细胞表达哺乳动物I型PLA2的高亲和力结合位点,在4℃下测得的解离常数(KD)为6.4 nM,最大结合量(Bmax)为0.1 - 1 pmol/mg DNA,分子量约为200 kDa。当UIII细胞在37℃下用I型PLA2处理时,与细胞特异性结合的配体增加,孵育90分钟后达到平台期,其水平比细胞维持在4℃时测得的水平高约5倍。我们可以确定PLA2与负责配体内化的质膜受体结合,并且在UIII细胞于37℃孵育期间,结合位点在质膜水平仍适合结合。仅在UIII细胞与配体于37℃孵育90分钟后才能清楚地检测到内化PLA2的蛋白水解,并且大多数细胞内PLA2由明显完整的14 kDa酶组成。通过交联研究,我们发现大多数内化的PLA2不与受体相关,支持了在我们的实验系统中,哺乳动物I型PLA2的单一膜受体池经历配体结合、细胞内转运和PLA2释放的循环,随后质膜上的结合位点得以恢复的结论。我们计算出在37℃下UIII细胞中一个受体分子内化配体的速率约为每小时三个I型PLA2分子。