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'''C16''' ('''PKRi''', '''GW 506033X''') is a drug which acts as a selective [[enzyme inhibition|inhibitor]] of the enzyme [[double-stranded RNA-dependent protein kinase]] (PKR). It has been shown to effectively inhibit PKR function ''in vivo'' and has [[neuroprotective]] and [[nootropic]] effects in animal studies.<ref>{{cite journal | last1 = Jammi | first1 = NV | last2 = Whitby | first2 = LR | last3 = Beal | first3 = PA | date = Aug 2003 | title = Small molecule inhibitors of the RNA-dependent protein kinase | url = | journal = Biochemical and Biophysical Research Communications | volume = 308 | issue = 1| pages = 50–7 | pmid = 12890478 | doi = 10.1016/s0006-291x(03)01318-4 }}</ref><ref>{{cite journal | last1 = Shimazawa | first1 = M | last2 = Hara | first2 = H | date = Dec 2006 | title = Inhibitor of double stranded RNA-dependent protein kinase protects against cell damage induced by ER stress | url = | journal = Neuroscience Letters | volume = 409 | issue = 3| pages = 192–5 | pmid = 17055645 | doi = 10.1016/j.neulet.2006.09.074 }}</ref><ref>{{Cite journal | last1 = Ingrand | first1 = S. | last2 = Barrier | first2 = L. | last3 = Lafay-Chebassier | first3 = C. | last4 = Fauconneau | first4 = B. | last5 = Page | first5 = G. N. | last6 = Hugon | first6 = J. | doi = 10.1016/j.febslet.2007.08.022 | title = The oxindole/imidazole derivative C16 reduces in vivo brain PKR activation | journal = FEBS Letters | volume = 581 | issue = 23 | pages = 4473–4478 | year = 2007 | pmid = 17761171| pmc = }}</ref><ref>{{Cite journal | last1 = Chen | first1 = H. M. | last2 = Wang | first2 = L. | last3 = d'Mello | first3 = S. R. | doi = 10.1111/j.1460-9568.2008.06491.x | title = 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 | journal = European Journal of Neuroscience | volume = 28 | issue = 10 | pages = 2003–2016 | year = 2008 | pmid = 19046382| pmc = 3320856}}</ref><ref>{{cite journal | last1 = Couturier | first1 = J | last2 = Morel | first2 = M | last3 = Pontcharraud | first3 = R | last4 = Gontier | first4 = V | last5 = Fauconneau | first5 = B | last6 = Paccalin | first6 = M | last7 = Page | first7 = G | date = Jan 2010 | title = 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 = Journal of Biological Chemistry | volume = 285 | issue = 2| pages = 1272–82 | pmid = 19889624 | doi = 10.1074/jbc.M109.041954 | pmc = 2801255 }}</ref><ref>{{cite journal | vauthors = 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 | year = 2011 | title = Suppression of PKR Promotes Network Excitability and Enhanced Cognition by Interferon-γ-Mediated Disinhibition | journal = Cell | volume = 147 | issue = 6 | pages = 1384–1396 | doi = 10.1016/j.cell.2011.11.029 | url = | accessdate = | pmid=22153080 | pmc=3569515}}</ref>
'''C16''' ('''PKRi''', '''GW 506033X''') is a drug which acts as a selective [[enzyme inhibition|inhibitor]] of the enzyme [[double-stranded RNA-dependent protein kinase]] (PKR). It has been shown to effectively inhibit PKR function ''in vivo'' and has [[neuroprotective]] and [[nootropic]] effects in animal studies.<ref>{{cite journal | last1 = Jammi | first1 = NV | last2 = Whitby | first2 = LR | last3 = Beal | first3 = PA | date = Aug 2003 | title = Small molecule inhibitors of the RNA-dependent protein kinase | url = | journal = Biochemical and Biophysical Research Communications | volume = 308 | issue = 1| pages = 50–7 | pmid = 12890478 | doi = 10.1016/s0006-291x(03)01318-4 }}</ref><ref>{{cite journal | last1 = Shimazawa | first1 = M | last2 = Hara | first2 = H | date = Dec 2006 | title = Inhibitor of double stranded RNA-dependent protein kinase protects against cell damage induced by ER stress | url = | journal = Neuroscience Letters | volume = 409 | issue = 3| pages = 192–5 | pmid = 17055645 | doi = 10.1016/j.neulet.2006.09.074 }}</ref><ref>{{Cite journal | last1 = Ingrand | first1 = S. | last2 = Barrier | first2 = L. | last3 = Lafay-Chebassier | first3 = C. | last4 = Fauconneau | first4 = B. | last5 = Page | first5 = G. N. | last6 = Hugon | first6 = J. | doi = 10.1016/j.febslet.2007.08.022 | title = The oxindole/imidazole derivative C16 reduces in vivo brain PKR activation | journal = FEBS Letters | volume = 581 | issue = 23 | pages = 4473–4478 | year = 2007 | pmid = 17761171| pmc = }}</ref><ref>{{Cite journal | last1 = Chen | first1 = H. M. | last2 = Wang | first2 = L. | last3 = d'Mello | first3 = S. R. | doi = 10.1111/j.1460-9568.2008.06491.x | title = 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 | journal = European Journal of Neuroscience | volume = 28 | issue = 10 | pages = 2003–2016 | year = 2008 | pmid = 19046382| pmc = 3320856}}</ref><ref>{{cite journal | last1 = Couturier | first1 = J | last2 = Morel | first2 = M | last3 = Pontcharraud | first3 = R | last4 = Gontier | first4 = V | last5 = Fauconneau | first5 = B | last6 = Paccalin | first6 = M | last7 = Page | first7 = G | date = Jan 2010 | title = 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 = Journal of Biological Chemistry | volume = 285 | issue = 2| pages = 1272–82 | pmid = 19889624 | doi = 10.1074/jbc.M109.041954 | pmc = 2801255 }}</ref><ref>{{cite journal | vauthors = 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 | year = 2011 | title = Suppression of PKR Promotes Network Excitability and Enhanced Cognition by Interferon-γ-Mediated Disinhibition | journal = Cell | volume = 147 | issue = 6 | pages = 1384–1396 | doi = 10.1016/j.cell.2011.11.029 | url = | accessdate = | pmid=22153080 | pmc=3569515}}</ref><ref>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}}</ref><ref>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}}</ref>


==See also==
==See also==

Revision as of 10:43, 5 August 2020

C16
Identifiers
  • 6,8-Dihydro-8-(1H-imidazol-5-ylmethylene)-7H-pyrrolo[2,3-g]benzothiazol-7-one
CAS Number
PubChem CID
ChemSpider
ECHA InfoCard100.211.648 Edit this at Wikidata
Chemical and physical data
FormulaC13H8N4OS
Molar mass268.29 g·mol−1
3D model (JSmol)
  • O=c3[nH]c2ccc1ncsc1c2c3=Cc4c[nH]cn4
  • 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 (PKRi, GW 506033X) is a drug which acts as a selective inhibitor of the enzyme double-stranded RNA-dependent protein kinase (PKR). It has been shown to effectively inhibit PKR function in vivo and has neuroprotective and nootropic effects in animal studies.[1][2][3][4][5][6][7][8]

See also

References

  1. ^ Jammi, NV; Whitby, LR; Beal, PA (Aug 2003). "Small molecule inhibitors of the RNA-dependent protein kinase". Biochemical and Biophysical Research Communications. 308 (1): 50–7. doi:10.1016/s0006-291x(03)01318-4. PMID 12890478.
  2. ^ Shimazawa, M; Hara, H (Dec 2006). "Inhibitor of double stranded RNA-dependent protein kinase protects against cell damage induced by ER stress". Neuroscience Letters. 409 (3): 192–5. doi:10.1016/j.neulet.2006.09.074. PMID 17055645.
  3. ^ Ingrand, S.; Barrier, L.; Lafay-Chebassier, C.; Fauconneau, B.; Page, G. N.; Hugon, J. (2007). "The oxindole/imidazole derivative C16 reduces in vivo brain PKR activation". FEBS Letters. 581 (23): 4473–4478. doi:10.1016/j.febslet.2007.08.022. PMID 17761171.
  4. ^ Chen, H. M.; Wang, L.; d'Mello, S. R. (2008). "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. 28 (10): 2003–2016. doi:10.1111/j.1460-9568.2008.06491.x. PMC 3320856. PMID 19046382.
  5. ^ Couturier, J; Morel, M; Pontcharraud, R; Gontier, V; Fauconneau, B; Paccalin, M; Page, G (Jan 2010). "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. 285 (2): 1272–82. doi:10.1074/jbc.M109.041954. PMC 2801255. PMID 19889624.{{cite journal}}: CS1 maint: unflagged free DOI (link)
  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 (2011). "Suppression of PKR Promotes Network Excitability and Enhanced Cognition by Interferon-γ-Mediated Disinhibition". Cell. 147 (6): 1384–1396. doi:10.1016/j.cell.2011.11.029. PMC 3569515. PMID 22153080.
  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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