Vu Han N, Situ Alan J, Dai Xuhang, Ulmer Tobias S
Department of Physiology and Neuroscience, Zilkha Neurogenetic Institute, Keck School of Medicine, University of Southern California, Los Angeles, California 90033, United States.
Biochemistry. 2025 Apr 1;64(7):1450-1462. doi: 10.1021/acs.biochem.4c00864. Epub 2025 Mar 11.
In the innate immune system, the CD33 receptor modulates microglial activity. Its downregulation promises to slow Alzheimer's disease, and it is already targeted in blood cancers. The mechanism underlying CD33 signaling is unresolved. Starting from the available crystal structure of its extracellular IgV-IgC1 domains, we have assembled a model of the human CD33 receptor by characterizing the oligomerization and structure of IgC1, transmembrane, and cytosolic domains in solution. IgC1 homodimerizes via intermolecular β-strand pairing and packing. In contrast, the 21-residue transmembrane helix of CD33 appears monomeric and straight, with a conserved thin neck and thick belly appearance followed by a positively charged cytosolic patch. The cytosolic domain is dynamically unstructured. Sequence alignment and AlphaFold models indicate that IgC domains in the family of human Siglecs, to which CD33 belongs, are surprisingly variable. Only Siglec-6 is identified to analogously dimerize via IgC1. Our CD33 structural model suggests that the receptor is not signaling via a monomer-dimer shift. Rather, we propose that, aided but also constrained by dimerization, multivalent ligands may concentrate the receptor transmembrane and cytosolic domains sufficiently to trigger colocalization with an activating kinase.
在先天免疫系统中,CD33受体调节小胶质细胞的活性。其下调有望减缓阿尔茨海默病的进程,并且它已经是血液癌症的治疗靶点。CD33信号传导的潜在机制尚未明确。基于其细胞外IgV-IgC1结构域的现有晶体结构,我们通过表征溶液中IgC1、跨膜和胞质结构域的寡聚化和结构,构建了人类CD33受体的模型。IgC1通过分子间β链配对和堆积形成同型二聚体。相比之下,CD33的21个残基跨膜螺旋呈单体且笔直状态,具有保守的细颈和粗腹外观,随后是带正电荷的胞质区域。胞质结构域是动态无序的。序列比对和AlphaFold模型表明,CD33所属的人类唾液酸结合免疫球蛋白样凝集素(Siglec)家族中的IgC结构域具有惊人的变异性。仅发现Siglec-6通过IgC1类似地形成二聚体。我们的CD33结构模型表明,该受体并非通过单体-二聚体转变进行信号传导。相反,我们提出,在二聚化的辅助和限制下,多价配体可能会充分聚集受体的跨膜和胞质结构域,从而触发与激活激酶的共定位。