Lo W W, Hughes J
Parke-Davis Research Unit, Addenbrookes Hospital Site, Cambridge, U.K.
Neurosci Lett. 1987 Oct 29;81(3):331-4. doi: 10.1016/0304-3940(87)90405-8.
Specific binding sites for inositol-(1,4,5)-trisphosphate (IP3) were demonstrated in rat cerebral cortical microsomal membranes using [3H]IP3 as the ligand. The binding was displaceable (IC50 for IP3 = 28 nM), high affinity (Kd = 20 nM) and saturable (Bmax = 7.75 pmol/mg protein). Kinetic studies showed an extremely rapid time-course of [3H]IP3 binding with half-maximal binding achieved in less than 1 min and equilibrium binding was attained by around 5 min. These results are in accord with the proposed function of IP3 in mobilizing intracellular calcium from endoplasmic reticulum.
以[3H]肌醇-(1,4,5)-三磷酸(IP3)作为配体,在大鼠大脑皮质微粒体膜中证实了IP3的特异性结合位点。该结合是可置换的(IP3的IC50 = 28 nM)、高亲和力的(Kd = 20 nM)且可饱和的(Bmax = 7.75 pmol/mg蛋白质)。动力学研究表明,[3H]IP3结合具有极快的时间进程,不到1分钟即可达到最大结合量的一半,约5分钟达到平衡结合。这些结果与IP3在内质网中动员细胞内钙的 proposed 功能一致。 (注:原文中“proposed”翻译为“推测的,假定的”,这里可能是根据语境灵活处理为“所提出的”更通顺些,但严格按要求保留原文形式)