Ilondo M M, Courtoy P J, Geiger D, Carpentier J L, Rousseau G G, De Meyts P
Proc Natl Acad Sci U S A. 1986 Sep;83(17):6460-4. doi: 10.1073/pnas.83.17.6460.
We have investigated whether the slowly dissociating component of insulin and human growth hormone (hGH) binding and the homologous down-regulation of their receptors in IM-9 cultured human lymphocytes are due to distinct conformations of the receptor or, rather, to a redistribution within the cell. To do so, we used intracellular K+ depletion, which has been shown to inhibit reversibly coated-pit formation and ligand internalization in some cell lines. IM-9 cells incubated in K+-free buffer after a hypotonic shock rapidly lost their K+, which was stabilized at +/- 50% of control by incubation in K+-free binding assay buffer. In K+-depleted cells, the hGH dissociation kinetics became monoexponential and, in contrast with control cells, compatible with the equilibrium constant derived from saturation and association data using a simple model. The loss of hGH receptors during competition studies was abolished. The down-regulation by unlabeled hGH was decreased by 80%. In contrast, insulin receptor kinetics remained unchanged (non-first-order) in the K+-depleted cells; the negative cooperativity and the down-regulation (60%) were identical to those of control cells. Quantitative electron microscopic autoradiography showed a decrease of +/- 50% in the fraction of 125I-labeled hGH internalized. The number of visible coated pits in the membrane was reduced by 80%. Thus, in IM-9 cells, association with coated pits and endocytosis appear to play a major role in the kinetics of hGH binding and in the down-regulation of its receptors, but not in insulin-receptor binding kinetics and down-regulation.
我们研究了胰岛素和人生长激素(hGH)结合的缓慢解离成分以及它们在IM-9培养的人淋巴细胞中受体的同源性下调是由于受体的不同构象,还是由于细胞内的重新分布。为此,我们使用了细胞内钾离子耗竭法,该方法已被证明可在某些细胞系中可逆地抑制有被小窝的形成和配体内化。在低渗休克后于无钾缓冲液中孵育的IM-9细胞迅速失去其钾离子,通过在无钾结合测定缓冲液中孵育,钾离子稳定在对照的±50%。在钾离子耗竭的细胞中,hGH的解离动力学变为单指数形式,与对照细胞相反,使用简单模型与从饱和及结合数据推导的平衡常数相符。在竞争研究中hGH受体的丢失被消除。未标记的hGH引起的下调减少了80%。相比之下,在钾离子耗竭的细胞中胰岛素受体动力学保持不变(非一级动力学);负协同性和下调(60%)与对照细胞相同。定量电子显微镜放射自显影显示内化的125I标记hGH的比例下降了±50%。膜中可见有被小窝的数量减少了80%。因此,在IM-9细胞中,与有被小窝的结合和内吞作用似乎在hGH结合动力学及其受体的下调中起主要作用,但在胰岛素受体结合动力学和下调中不起作用。