| 靶标 | Sigma-2 receptor, Sigma intracellular receptor 2, Meningioma-associated protein 30, MAC30, Transmembrane protein 97, S2R, TMEM97, Sigma2 receptor |
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| 背景 | Sigma intracellular receptor 2 (TMEM97) is a ~20 kDa protein. Sigma-2 receptor which contributes to ameliorate dysfunctional cellular processes and slow degenerative progression by regulating cell functions including cholesterol biosynthesis/trafficking, membrane trafficking, autophagy, lipid membrane-bound protein trafficking, and receptor stabilization at the cell surface (Probable). Forms a ternary complex with PGRMC1 receptor and low density lipoprotein receptor/LDLR at the plasma membrane, which increases LDLR-mediated LDL cholesterol internalization. Decreases lysosomal sterol transporter NPC1 availability to the cell, probably through NPC1-binding, hence controlling lipid transport, including cholesterol and LBPA, outside of late endosome/lysosome. Binds regio- and stereoselective ligand 20(S)-hydroxycholesterol (20(S)-OHC) which enhances TMEM97-NPC1 interaction and decreases TMEM97-PGRMC1 and TMEM97-TSPO interactions, thereby linking OHC binding to cholesterol homeostasis. Also able to bind cholesterol. 2. Huang, YS. et al. (2014) Medicinal research reviews 34, 532-66. PMID: 239222153. Guo, L. et al. (2015) Current medicinal chemistry 22, 989-1003. PMID: 256200954. Ebrahimi-Fakhari, D. et al. (2016) Human molecular genetics 25, 3588-3599. PMID: 273786905. Alon, A. et al. (2017) Proceedings of the National Academy of Sciences of the United States of America 114, 7160-7165. PMID: 285593377. Son, KN. et al. (2021) The FEBS journal 288, 6815-6827. PMID: 342330618. Cheng, YS. et al. (2021) Nature chemical biology 17, 1271-1280. PMID: 347997359. Ma, D. et al. (2022) International journal of oral science 14, 42. PMID: 35970844 |
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