C16 (药物)

C16
识别信息
	IUPAC命名法 6,8-Dihydro-8-(1H-imidazol-5-ylmethylene)-7H-pyrrolo[2,3-g]benzothiazol-7-one; ;
CAS号	608512-97-6
PubChem CID	6490494;
ChemSpider	4990932;
UNII	C9Q75QZK84;
ECHA InfoCard	100.211.648
化学信息
化学式	C13H8N4OS
摩尔质量	268.29 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES O=c3[nH]c2ccc1ncsc1c2c3=Cc4c[nH]cn4;
	InChI InChI=1S/C13H8N4OS/c18-13-8(3-7-4-14-5-15-7)11-9(17-13)1-2-10-12(11)19-6-16-10/h1-6H,(H,14,15)(H,17,18)/b8-3-; Key:VFBGXTUGODTSPK-BAQGIRSFSA-N;

C16（也称为PKRi或GW 506033X）是一种蛋白激酶R（PKR，也称为双链RNA依赖性蛋白激酶）的选择性酶抑制剂。^[1]^[2]^[3]^[4]^[5]^[6]^[7]^[8]

参考文献

^ Jammi, NV; Whitby, LR; Beal, PA. Small molecule inhibitors of the RNA-dependent protein kinase. Biochemical and Biophysical Research Communications. Aug 2003, 308 (1): 50–7. PMID 12890478. doi:10.1016/s0006-291x(03)01318-4.
^ Shimazawa, M; Hara, H. Inhibitor of double stranded RNA-dependent protein kinase protects against cell damage induced by ER stress. Neuroscience Letters. Dec 2006, 409 (3): 192–5. PMID 17055645. S2CID 43133290. doi:10.1016/j.neulet.2006.09.074.
^ Ingrand, S.; Barrier, L.; Lafay-Chebassier, C.; Fauconneau, B.; Page, G. N.; Hugon, J. The oxindole/imidazole derivative C16 reduces in vivo brain PKR activation. FEBS Letters. 2007, 581 (23): 4473–4478. PMID 17761171. doi:10.1016/j.febslet.2007.08.022 .
^ Chen, H. M.; Wang, L.; d'Mello, S. R. A chemical compound commonly used to inhibit PKR, {8-(imidazol-4-ylmethylene)-6H-azolidino[5,4-g] benzothiazol-7-one}, protects neurons by inhibiting cyclin-dependent kinase. European Journal of Neuroscience. 2008, 28 (10): 2003–2016. PMC 3320856 . PMID 19046382. doi:10.1111/j.1460-9568.2008.06491.x.
^ Couturier, J; Morel, M; Pontcharraud, R; Gontier, V; Fauconneau, B; Paccalin, M; Page, G. Interaction of double-stranded RNA-dependent protein kinase (PKR) with the death receptor signaling pathway in amyloid beta (Abeta)-treated cells and in APPSLPS1 knock-in mice. Journal of Biological Chemistry. Jan 2010, 285 (2): 1272–82. PMC 2801255 . PMID 19889624. doi:10.1074/jbc.M109.041954 .
^ Zhu PJ, Huang W, Kalikulov D, Yoo JW, Placzek AN, Stoica L, Zhou H, Bell JC, Friedlander MJ, Krnjevic K, Noebels JL, Costa-Mattioli M. Suppression of PKR Promotes Network Excitability and Enhanced Cognition by Interferon-γ-Mediated Disinhibition. Cell. 2011, 147 (6): 1384–1396. PMC 3569515 . PMID 22153080. doi:10.1016/j.cell.2011.11.029.
^ Hwang KD, Bak MS, Kim SJ, Rhee S, Lee YS. Restoring synaptic plasticity and memory in mouse models of Alzheimer's disease by PKR inhibition. Mol Brain. 2017;10(1):57. doi:10.1186/s13041-017-0338-3
^ Gal-Ben-Ari S, Barrera I, Ehrlich M, Rosenblum K. PKR: A Kinase to Remember. Front Mol Neurosci. 2019;11:480. doi:10.3389/fnmol.2018.00480

[1] Jammi, NV; Whitby, LR; Beal, PA. Small molecule inhibitors of the RNA-dependent protein kinase. Biochemical and Biophysical Research Communications. Aug 2003, 308 (1): 50–7. PMID 12890478. doi:10.1016/s0006-291x(03)01318-4.

[2] Shimazawa, M; Hara, H. Inhibitor of double stranded RNA-dependent protein kinase protects against cell damage induced by ER stress. Neuroscience Letters. Dec 2006, 409 (3): 192–5. PMID 17055645. S2CID 43133290. doi:10.1016/j.neulet.2006.09.074.

[3] Ingrand, S.; Barrier, L.; Lafay-Chebassier, C.; Fauconneau, B.; Page, G. N.; Hugon, J. The oxindole/imidazole derivative C16 reduces in vivo brain PKR activation. FEBS Letters. 2007, 581 (23): 4473–4478. PMID 17761171. doi:10.1016/j.febslet.2007.08.022 .

[4] Chen, H. M.; Wang, L.; d'Mello, S. R. A chemical compound commonly used to inhibit PKR, {8-(imidazol-4-ylmethylene)-6H-azolidino[5,4-g] benzothiazol-7-one}, protects neurons by inhibiting cyclin-dependent kinase. European Journal of Neuroscience. 2008, 28 (10): 2003–2016. PMC 3320856 . PMID 19046382. doi:10.1111/j.1460-9568.2008.06491.x.

[5] Couturier, J; Morel, M; Pontcharraud, R; Gontier, V; Fauconneau, B; Paccalin, M; Page, G. Interaction of double-stranded RNA-dependent protein kinase (PKR) with the death receptor signaling pathway in amyloid beta (Abeta)-treated cells and in APPSLPS1 knock-in mice. Journal of Biological Chemistry. Jan 2010, 285 (2): 1272–82. PMC 2801255 . PMID 19889624. doi:10.1074/jbc.M109.041954 .

[6] Zhu PJ, Huang W, Kalikulov D, Yoo JW, Placzek AN, Stoica L, Zhou H, Bell JC, Friedlander MJ, Krnjevic K, Noebels JL, Costa-Mattioli M. Suppression of PKR Promotes Network Excitability and Enhanced Cognition by Interferon-γ-Mediated Disinhibition. Cell. 2011, 147 (6): 1384–1396. PMC 3569515 . PMID 22153080. doi:10.1016/j.cell.2011.11.029.

[7] Hwang KD, Bak MS, Kim SJ, Rhee S, Lee YS. Restoring synaptic plasticity and memory in mouse models of Alzheimer's disease by PKR inhibition. Mol Brain. 2017;10(1):57. doi:10.1186/s13041-017-0338-3

[8] Gal-Ben-Ari S, Barrera I, Ehrlich M, Rosenblum K. PKR: A Kinase to Remember. Front Mol Neurosci. 2019;11:480. doi:10.3389/fnmol.2018.00480

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