GSK-4112 is an experimental drug that was developed by GlaxoSmithKline as an agonist of Rev-ErbAα.[1] It is used for studying regulation of the circadian rhythm and its influence on diverse processes such as adipogenesis,[2][3] regulation of bone density,[4] and inflammation.[5][6][7][8]
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Formula | C18H21ClN2O4S |
Molar mass | 396.89 g·mol−1 |
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See also
editReferences
edit- ^ Grant D, Yin L, Collins JL, Parks DJ, Orband-Miller LA, Wisely GB, et al. (October 2010). "GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα". ACS Chemical Biology. 5 (10): 925–32. doi:10.1021/cb100141y. PMID 20677822.
- ^ Kojetin DJ, Burris TP (2011). "A role for rev-erbα ligands in regulation of adipogenesis". Current Pharmaceutical Design. 17 (4): 320–4. doi:10.2174/138161211795164211. PMID 21375499.
- ^ Chu G, Zhou X, Hu Y, Shi S, Yang G (September 2019). "Rev-erbα Inhibits Proliferation and Promotes Apoptosis of Preadipocytes through the Agonist GSK4112". International Journal of Molecular Sciences. 20 (18): 4524. doi:10.3390/ijms20184524. PMC 6769707. PMID 31547330.
- ^ Kim K, Kim JH, Kim I, Seong S, Kim N (January 2020). "Rev-erbα Negatively Regulates Osteoclast and Osteoblast Differentiation through p38 MAPK Signaling Pathway". Molecules and Cells. 43 (1): 34–47. doi:10.14348/molcells.2019.0232. PMC 6999712. PMID 31896234.
- ^ Sato S, Sakurai T, Ogasawara J, Takahashi M, Izawa T, Imaizumi K, et al. (January 2014). "A circadian clock gene, Rev-erbα, modulates the inflammatory function of macrophages through the negative regulation of Ccl2 expression". Journal of Immunology. 192 (1): 407–17. doi:10.4049/jimmunol.1301982. PMID 24307731.
- ^ Sundar IK, Rashid K, Sellix MT, Rahman I (December 2017). "The nuclear receptor and clock gene REV-ERBα regulates cigarette smoke-induced lung inflammation". Biochemical and Biophysical Research Communications. 493 (4): 1390–1395. doi:10.1016/j.bbrc.2017.09.157. PMC 5756581. PMID 28974420.
- ^ Guo DK, Zhu Y, Sun HY, Xu XY, Zhang S, Hao ZB, et al. (January 2019). "Pharmacological activation of REV-ERBα represses LPS-induced microglial activation through the NF-κB pathway". Acta Pharmacologica Sinica. 40 (1): 26–34. doi:10.1038/s41401-018-0064-0. PMC 6318300. PMID 29950615.
- ^ Morioka N, Kodama K, Tomori M, Yoshikawa K, Saeki M, Nakamura Y, et al. (May 2019). "Stimulation of nuclear receptor REV-ERBs suppresses production of pronociceptive molecules in cultured spinal astrocytes and ameliorates mechanical hypersensitivity of inflammatory and neuropathic pain of mice" (PDF). Brain, Behavior, and Immunity. 78: 116–130. doi:10.1016/j.bbi.2019.01.014. PMID 30682503. S2CID 59273997.