Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
Electrophilic compounds originating from nature or chemical synthesis have profound effects on immune cells. These compounds are thought to act by cysteine modification to alter the functions of immune-relevant proteins; however, our understanding of electrophile-sensitive cysteines in the human immune proteome remains limited. Here, we present a global map of cysteines in primary human T cells that are susceptible to covalent modification by electrophilic small molecules. More than 3,000 covalently liganded cysteines were found on functionally and structurally diverse proteins, including many that play fundamental roles in immunology. We further show that electrophilic compounds can impair T cell activation by distinct mechanisms involving the direct functional perturbation and/or degradation of proteins. Our findings reveal a rich content of ligandable cysteines in human T cells and point to electrophilic small molecules as a fertile source for chemical probes and ultimately therapeutics that modulate immunological processes and their associated disorders.
天然或化学合成的亲电化合物对免疫细胞有深远的影响。这些化合物被认为通过半胱氨酸修饰来改变与免疫相关的蛋白质的功能;然而,我们对人类免疫蛋白质组中亲电敏感半胱氨酸的理解仍然有限。在这里,我们呈现了原发性人 T 细胞中易受亲电小分子共价修饰的半胱氨酸的全局图谱。在功能和结构上多样化的蛋白质上发现了 3000 多个共价连接的半胱氨酸,其中包括许多在免疫学中起基本作用的蛋白质。我们进一步表明,亲电化合物可以通过涉及蛋白质的直接功能干扰和/或降解的不同机制来损害 T 细胞的激活。我们的发现揭示了人类 T 细胞中丰富的可配体半胱氨酸含量,并指出亲电小分子是化学探针的丰富来源,最终可用于调节免疫过程及其相关疾病的治疗药物。