Chemistry:Salubrinal
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Short description: Chemical compound
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| Formula | C21H17Cl3N4OS |
| Molar mass | 479.80 g·mol−1 |
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Salubrinal is a drug which acts as a specific inhibitor of eIF2α phosphatase enzymes[1][2][3] and is primarily used experimentally, to study stress responses in eukaryotic cells associated with the action of eIF2. Salubrinal indirectly inhibits eIF2 as a result of reduced dephosphorylation of its α-subunit,[4] resulting in activation of stress response pathways usually triggered by events such as oxidative stress or buildup of unfolded protein in the endoplasmic reticulum.[5] Salubrinal has putative therapeutic value due to its function,[1][3] but is as yet only used experimentally. Salubrinal is being studied at Indiana University for its potential to fight osteoporosis and accelerate bone healing.[6]
References
- ↑ 1.0 1.1 "Basal levels of eIF2alpha phosphorylation determine cellular antioxidant status by regulating ATF4 and xCT expression". The Journal of Biological Chemistry (The American Society for Biochemistry and Molecular Biology, Inc) 284 (2): 1106–15. January 2009. doi:10.1074/jbc.M807325200. PMID 19017641.
- ↑ "Protection of Bcl-2 by salubrinal". Biochemical and Biophysical Research Communications (Elsevier Inc) 346 (4): 1320–3. August 2006. doi:10.1016/j.bbrc.2006.06.056. PMID 16806073.
- ↑ 3.0 3.1 "A selective inhibitor of eIF2alpha dephosphorylation protects cells from ER stress". Science 307 (5711): 935–9. February 2005. doi:10.1126/science.1101902. PMID 15705855. Bibcode: 2005Sci...307..935B. http://www.sciencemag.org/cgi/content/abstract/307/5711/935.
- ↑ "Entrez Gene: EIF2S1 eukaryotic translation initiation factor 2, subunit 1 alpha, 35kDa". National Center for Biotechnology Information, U.S. National Library of Medicine. https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=1965.
- ↑ "Coping with stress: eIF2 kinases and translational control". Biochemical Society Transactions (Biochemical Society) 34 (Pt 1): 7–11. February 2006. doi:10.1042/BST20060007. PMID 16246168.
- ↑ "New compound may accelerate bone healing, prevent osteoporosis". August 2011. http://www.cloningresources.com/research/New_compound_may_accelerate_bone_healing_prevent_osteoporosis.asp.
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