Dalby Anders, Kaas Mathias, Meinertz Byg Lars, Christiansen Signe Bundgaard, Longworth Christian M, Hansen Simon Bøggild, Qvist Per, Nyengaard Jens R, Madsen Peder, Mølgaard Simon, Glerup Simon
Department of Biomedicine, Aarhus University, 8000 Aarhus, Denmark.
Teitur Trophics ApS, 8200 Aarhus, Denmark.
iScience. 2025 May 19;28(6):112695. doi: 10.1016/j.isci.2025.112695. eCollection 2025 Jun 20.
The Vps10p-domain receptors SorCS1-3 have been repeatedly associated with the development of neurological and psychiatric disorders. They have emerged as key regulators of synaptic activity and neurotrophic signaling, but the underlying molecular mechanism remains poorly understood. Here we report that the SorCS2 intracellular domain (ICD) contains a triple serine motif that potentially functions as a signaling switch to induce intracellular signaling in hippocampal neurons. We show, that serine to alanine substitution in this motif renders neurons less responsive to BDNF, whereas phosphomimetic mutations induce neurotrophic effects independently of the SorCS2 extracellular domain (ECD) and BDNF. Hence, we develop triple serine motif-based cell-penetrating peptides that modulate distinct intracellular signaling, partially overlapping with the BDNF pathway, ultimately activating the transcription factor CREB. Taken together, we provide insights into SorCS2 mediated neurotrophic signaling and use this knowledge to develop pharmacologically active molecules.
Vps10p结构域受体SorCS1 - 3多次被认为与神经和精神疾病的发生有关。它们已成为突触活动和神经营养信号传导的关键调节因子,但其潜在的分子机制仍知之甚少。在此,我们报告SorCS2细胞内结构域(ICD)包含一个三重丝氨酸基序,该基序可能作为信号开关,在海马神经元中诱导细胞内信号传导。我们发现,该基序中的丝氨酸被丙氨酸取代会使神经元对脑源性神经营因子(BDNF)的反应性降低,而模拟磷酸化的突变则可独立于SorCS2细胞外结构域(ECD)和BDNF诱导神经营养作用。因此,我们开发了基于三重丝氨酸基序的细胞穿透肽,其可调节与BDNF途径部分重叠的不同细胞内信号传导,最终激活转录因子CREB。综上所述,我们深入了解了SorCS2介导的神经营养信号传导,并利用这些知识开发了具有药理活性的分子。