TSPO ligand-1 是 AUTAC4 的配体，可用于合成 PROTACs。TSPO ligand-1 是一种线粒体外膜跨膜结构域蛋白，可与 AUTAC4 相结合，调节线粒体自噬 (autophagy) 促进靶向线粒体更新。TSPO ligand-1 也可参与胆固醇从线粒体外膜到内膜的转运，作为脑损伤和神经变性的敏感生物标志物。
TSPO ligand-1 is the ligand of AUTAC4 (cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration[1][2].
TSPO ligand-1 gene is induced to increase expression in the context of selective activation of neurons in male C57Bl6/N mice. Moreover, neuronal activation under psiological and psychopharmacological conditions also results in increased TSPO levels in adult mice[2].
TSPO ligand-1 can serve as the sole marker of glial cell activity in Alzheimer's disease thus tracking the formation of different neural cells[3].
TSPO ligand-1 can regulate mitochondrial fatty acid oxidation (FAO) and thus effects mitochondrial energy homeostasis in MA-10 Leydig cell line[4].
[1]. Takahashi D, et, al. AUTACs: Cargo-Specific Degraders Using Selective Autophagy. Mol Cell. 2019 Dec 5;76(5):797-810.e10.
[2]. Tina Notter, et al. Neuronal activity increases translocator protein (TSPO) levels. Mol Psychiatry. 2021 Jun;26(6):2025-2037. doi: 10.1038/s41380-020-0745-1. Epub 2020 May 12.
[3]. Benjamin B Tournier, et al. Astrocytic TSPO Upregulation Appears Before Microglial TSPO in Alzheimer's Disease. J Alzheimers Dis. 2020;77(3):1043-1056. doi: 10.3233/JAD-200136.
[4]. Lan N Tu, et al. Translocator Protein (TSPO) Affects Mitochondrial Fatty Acid Oxidation in Steroidogenic Cells. Endocrinology. 2016 Mar;157(3):1110-21. doi: 10.1210/en.2015-1795. Epub 2016 Jan 7.
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