Department of Biology, Indiana University-Purdue University, Indianapolis, Indiana, USA.
Department of Medical and Molecular Genetics, Indiana University School of Medicine, Indianapolis, Indiana, USA.
J Neurochem. 2019 Oct;151(2):185-203. doi: 10.1111/jnc.14831. Epub 2019 Aug 2.
N-methyl-d-Aspartate receptors (NMDARs) are abundant postsynaptic proteins that are critical for normal synaptic communication. NMDAR channel function is regulated by multiple properties, including phosphorylation. Inhibition of protein phosphatase 1 (PP1) in hippocampal neurons increases NMDAR activity, an effect abrogated by loss of spinophilin, the major PP1-targeting protein in the postsynaptic density. However, how spinophilin regulates PP1-dependent NMDAR function is unclear. We hypothesize that spinophilin regulates PP1 binding to the NMDAR to alter NMDAR phosphorylation. Our data demonstrate that spinophilin interacts with the GluN2B subunit of the NMDAR. In human embryonic kidney 293 FT cells, activation and/or overexpression of protein kinase A increased the association between spinophilin and the GluN2B subunit of the NMDAR. Functionally, we found that spinophilin overexpression decreased PP1 binding to the GluN2B subunit of the NMDAR and attenuated the PP1-dependent dephosphorylation of GluN2B at Ser-1284. Moreover, in P28 hippocampal lysates isolated from spinophilin KO compared to WT mice, there was increased binding of GluN2B to PP1, decreased phosphorylation of GluN2B at Ser-1284, and altered GluN2B protein interactions with postsynaptic density-enriched proteins. Together, our data demonstrate that spinophilin decreases PP1 binding to GluN2B and concomitantly enhances the phosphorylation of GluN2B at Ser-1284. The putative consequences of these spinophilin-dependent alterations in GluN2B phosphorylation and interactions on synaptic GluN2B localization and function are discussed. Open Science: This manuscript was awarded with the Open Materials Badge For more information see: https://cos.io/our-services/open-science-badges/.
N-甲基-D-天冬氨酸受体(NMDARs)是丰富的突触后蛋白,对正常的突触通讯至关重要。NMDAR 通道功能受多种特性调节,包括磷酸化。在海马神经元中抑制蛋白磷酸酶 1(PP1)会增加 NMDAR 活性,而这种作用被突触后密度中主要的 PP1 靶向蛋白 spinophilin 的缺失所阻断。然而,spinophilin 如何调节依赖于 PP1 的 NMDAR 功能尚不清楚。我们假设 spinophilin 通过调节 PP1 与 NMDAR 的结合来改变 NMDAR 的磷酸化。我们的数据表明,spinophilin 与 NMDAR 的 GluN2B 亚基相互作用。在人胚肾 293FT 细胞中,蛋白激酶 A 的激活和/或过表达增加了 spinophilin 与 NMDAR 的 GluN2B 亚基的结合。功能上,我们发现 spinophilin 的过表达减少了 PP1 与 NMDAR 的 GluN2B 亚基的结合,并减弱了 PP1 依赖性的 GluN2B 在 Ser-1284 上的去磷酸化。此外,与 WT 小鼠相比,从 spinophilin KO 小鼠的 P28 海马裂解物中,GluN2B 与 PP1 的结合增加,GluN2B 在 Ser-1284 上的磷酸化减少,并且 GluN2B 蛋白与突触后密度丰富蛋白的相互作用发生改变。总之,我们的数据表明 spinophilin 减少了 PP1 与 GluN2B 的结合,并同时增强了 GluN2B 在 Ser-1284 上的磷酸化。讨论了这些依赖于 spinophilin 的 GluN2B 磷酸化和相互作用变化对突触 GluN2B 定位和功能的潜在影响。开放科学:本文获得了开放材料徽章更多信息见:https://cos.io/our-services/open-science-badges/。