Bender Julia, Engeholm Maik, Ederer Marion S, Breu Johannes, Møller Thor C, Michalakis Stylianos, Rasko Tamas, Wanker Erich E, Biel Martin, Martinez Karen L, Wurst Wolfgang, Deussing Jan M
Max Planck Institute of Psychiatry, Department of Stress Neurobiology and Neurogenetics, Molecular Neurogenetics, Munich, Germany.
Max Planck Institute of Psychiatry, Munich, Germany.
PLoS One. 2015 Sep 9;10(9):e0136768. doi: 10.1371/journal.pone.0136768. eCollection 2015.
The corticotropin-releasing hormone receptor type 1 (CRHR1) plays an important role in orchestrating neuroendocrine, behavioral, and autonomic responses to stress. To identify molecules capable of directly modulating CRHR1 signaling, we performed a yeast-two-hybrid screen using the C-terminal intracellular tail of the receptor as bait. We identified several members of the membrane-associated guanylate kinase (MAGUK) family: postsynaptic density protein 95 (PSD95), synapse-associated protein 97 (SAP97), SAP102 and membrane associated guanylate kinase, WW and PDZ domain containing 2 (MAGI2). CRHR1 is co-expressed with the identified MAGUKs and with the additionally investigated PSD93 in neurons of the adult mouse brain and in primary hippocampal neurons, supporting the probability of a physiological interaction in vivo. The C-terminal PDZ (PSD-95, discs large, zona occludens 1) binding motif of CRHR1 is essential for its physical interaction with MAGUKs, as revealed by the CRHR1-STAVA mutant, which harbors a functionally impaired PDZ binding motif. The imitation of a phosphorylation at Thr413 within the PDZ binding motif also disrupted the interaction with MAGUKs. In contrast, distinct PDZ domains within the identified MAGUKs are involved in the interactions. Expression of CRHR1 in primary neurons demonstrated its localization throughout the neuronal plasma membrane, including the excitatory post synapse, where the receptor co-localized with PSD95 and SAP97. The co-expression of CRHR1 and respective interacting MAGUKs in HEK293 cells resulted in a clustered subcellular co-localization which required an intact PDZ binding motif. In conclusion, our study characterized the PDZ binding motif-mediated interaction of CRHR1 with multiple MAGUKs, which directly affects receptor function.
1型促肾上腺皮质激素释放激素受体(CRHR1)在协调神经内分泌、行为和自主应激反应中起重要作用。为了鉴定能够直接调节CRHR1信号传导的分子,我们以受体的C末端细胞内尾巴为诱饵进行了酵母双杂交筛选。我们鉴定出了膜相关鸟苷酸激酶(MAGUK)家族的几个成员:突触后致密蛋白95(PSD95)、突触相关蛋白97(SAP97)、SAP102以及含WW和PDZ结构域的膜相关鸟苷酸激酶2(MAGI2)。CRHR1与鉴定出的MAGUK以及另外研究的PSD93在成年小鼠脑神经元和原代海马神经元中共同表达,这支持了体内发生生理相互作用的可能性。CRHR1的C末端PDZ(PSD - 95、盘状大蛋白、紧密连接蛋白1)结合基序对于其与MAGUK的物理相互作用至关重要,这由携带功能受损的PDZ结合基序的CRHR1 - STAVA突变体揭示。PDZ结合基序内Thr413处磷酸化的模拟也破坏了与MAGUK的相互作用。相反,鉴定出的MAGUK内不同的PDZ结构域参与了相互作用。CRHR1在原代神经元中的表达表明其定位于整个神经元质膜,包括兴奋性突触后部位,该受体在那里与PSD95和SAP97共定位。CRHR1与各自相互作用的MAGUK在HEK293细胞中的共表达导致了亚细胞聚集共定位,这需要完整的PDZ结合基序。总之,我们的研究表征了CRHR1与多种MAGUK之间由PDZ结合基序介导的相互作用,这直接影响受体功能。