Chemistry:Torin-1

From HandWiki
Short description: Chemical compound
Torin-1
Torin1 structure.png
Identifiers
CAS Number
PubChem CID
ChemSpider
ChEBI
ChEMBL
Chemical and physical data
FormulaC35H28F3N5O2
Molar mass607.637 g·mol−1
3D model (JSmol)

Torin-1 is a drug which was one of the first non-rapalog derived inhibitors of the mechanistic target of rapamycin (mTOR) subtypes mTORC1 and mTORC2.[1][2][3] In animal studies it has anti-inflammatory,[4][5] anti-cancer,[6][7] and anti-aging properties,[8][9][10][11] and shows activity against neuropathic pain.[12][13][14]

References

  1. "Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h[1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer"]. Journal of Medicinal Chemistry 53 (19): 7146–55. October 2010. doi:10.1021/jm101144f. PMID 20860370. 
  2. "ATP-competitive inhibitors of mTOR: an update". Current Medicinal Chemistry 18 (20): 2995–3014. 2011. doi:10.2174/092986711796391651. PMID 21651476. 
  3. "Development of ATP-Competitive mTOR Inhibitors". MTOR. Methods in Molecular Biology. 821. 2012. pp. 447–60. doi:10.1007/978-1-61779-430-8_29. ISBN 978-1-61779-429-2. 
  4. "Inhibition of mTOR blocks the anti-inflammatory effects of glucocorticoids in myeloid immune cells". Blood 117 (16): 4273–83. April 2011. doi:10.1182/blood-2010-09-310888. PMID 21368289. 
  5. "Methoxyluteolin Inhibits Neuropeptide-stimulated Proinflammatory Mediator Release via mTOR Activation from Human Mast Cells". The Journal of Pharmacology and Experimental Therapeutics 361 (3): 462–471. June 2017. doi:10.1124/jpet.117.240564. PMID 28404689. 
  6. "Selective targeting of human colon cancer stem-like cells by the mTOR inhibitor Torin-1". Oncotarget 4 (11): 1948–62. November 2013. doi:10.18632/oncotarget.1310. PMID 24185040. 
  7. "Distinct signaling mechanisms of mTORC1 and mTORC2 in glioblastoma multiforme: a tale of two complexes". Advances in Biological Regulation 57: 64–74. January 2015. doi:10.1016/j.jbior.2014.09.004. PMID 25442674. 
  8. "Dual mTORC1/C2 inhibitors suppress cellular geroconversion (a senescence program)". Oncotarget 6 (27): 23238–48. September 2015. doi:10.18632/oncotarget.4836. PMID 26177051. 
  9. "Gerosuppression by pan-mTOR inhibitors". Aging 8 (12): 3535–3551. December 2016. doi:10.18632/aging.101155. PMID 28077803. 
  10. "Lifespan extension without fertility reduction following dietary addition of the autophagy activator Torin1 in Drosophila melanogaster". PLOS ONE 13 (1): e0190105. 2018. doi:10.1371/journal.pone.0190105. PMID 29329306. Bibcode2018PLoSO..1390105M. 
  11. "The mTORC1-autophagy pathway is a target for senescent cell elimination". Biogerontology 20 (3): 331–335. June 2019. doi:10.1007/s10522-019-09802-9. PMID 30798505. 
  12. "Systemic inhibition of the mammalian target of rapamycin (mTOR) pathway reduces neuropathic pain in mice". Pain 152 (11): 2582–95. November 2011. doi:10.1016/j.pain.2011.07.025. PMID 21917376. 
  13. "mTOR signaling intervention by Torin1 and XL388 in the insular cortex alleviates neuropathic pain". Neuroscience Letters 718: 134742. January 2020. doi:10.1016/j.neulet.2020.134742. PMID 31917234. 
  14. "Effects of mTOR inhibitors on neuropathic pain revealed by optical imaging of the insular cortex in rats". Brain Research 1733: 146720. April 2020. doi:10.1016/j.brainres.2020.146720. PMID 32061737. https://ir.ymlib.yonsei.ac.kr/bitstream/22282913/175518/1/T202000481.pdf.