4560-08-1

TSPO ligand-1 is the ligand of AUTAC4 (HY-134640) that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration[1][2].

[1] Takahashi D, et, al. AUTACs: Cargo-Specific Degraders Using Selective Autophagy. Mol Cell. 2019 Dec 5;76(5):797-810.e10. DOI:10.1016/j.molcel.2019.09.009
[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. DOI:10.1038/s41380-020-0745-1
[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. 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. DOI:10.1210/en.2015-1795