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Axten JM, Medina JR, Feng Y, Shu A, Romeril SP, Grant SW, et al. (August 2012). "Discovery of 7-methyl-5-(1-{acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolopyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase
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of various diseases including prion and
Alzheimer's diseases. Treatment with GSK2606414 was found to be neuroprotective in mice against damage caused by prions, and prevented the development of cognitive deficits and other clinical manifestations of prion disease. Extension of lifespan in treated
306:(PERK), which is involved in various processes relating to cancer and neurodegenerative disorders. GSK2606414 was found to be a potent and selective inhibitor of PERK, with good oral bioavailability and blood-brain barrier penetration. PERK mediates the
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mice was, however, not recorded. However, side effects such as weight loss and elevated blood glucose levels were also observed, likely due to unwanted inhibition of PERK in the pancreas gland, where it is involved in regulating insulin production.
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Moreno JA, Halliday M, Molloy C, Radford H, Verity N, Axten JM, et al. (October 2013). "Oral treatment targeting the unfolded protein response prevents neurodegeneration and clinical disease in prion-infected mice".
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InChI=1S/C24H20F3N5O/c1-31-12-18(21-22(28)29-13-30-23(21)31)15-5-6-19-16(11-15)7-8-32(19)20(33)10-14-3-2-4-17(9-14)24(25,26)27/h2-6,9,11-13H,7-8,10H2,1H3,(H2,28,29,30)
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1-pyrimidin-5-yl)indolin-1-yl]-2-(3-trifluoromethylphenyl)ethanone
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