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Volumn 18, Issue 2, 2008, Pages 653-656

Novel heterocycle-substituted pyrimidines as inhibitors of NF-κB transcription regulation related to TNF-α cytokine release

Author keywords

Anti inflammation; Glycogen synthase kinase 3 ; Heterocyclic fused ring; Nuclear factor B; TNF cytokine

Indexed keywords

DORAMAPIMOD; GLYCOGEN SYNTHASE KINASE 3 INHIBITOR; GLYCOGEN SYNTHASE KINASE 3BETA; IMMUNOGLOBULIN ENHANCER BINDING PROTEIN; PYRIMIDINE DERIVATIVE; TUMOR NECROSIS FACTOR ALPHA;

EID: 38149050566     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.11.064     Document Type: Article
Times cited : (13)

References (24)
  • 1
    • 4444376712 scopus 로고    scopus 로고
    • For recent reviews, see
    • For recent reviews, see. Hayden M.S., and Ghosh S. Genes Dev. 18 (2004) 2195
    • (2004) Genes Dev. , vol.18 , pp. 2195
    • Hayden, M.S.1    Ghosh, S.2
  • 19
    • 0035665719 scopus 로고    scopus 로고
    • The molecular modeling was performed with the Maestro software package from Schrodinger. The ligand was manually docked into the active site. Structural co-ordinates for the GSK-3 structure were taken from:
    • The molecular modeling was performed with the Maestro software package from Schrodinger. The ligand was manually docked into the active site. Structural co-ordinates for the GSK-3 structure were taken from:. Bax B., Carter P.S., Lewis C., Guy A.R., Bridges A., Tanner R., Pettman G., Mannix C., Culbert A.A., Brown M.J.B., Smith D.G., and Reith A.D. Structure 9 (2001) 1143
    • (2001) Structure , vol.9 , pp. 1143
    • Bax, B.1    Carter, P.S.2    Lewis, C.3    Guy, A.R.4    Bridges, A.5    Tanner, R.6    Pettman, G.7    Mannix, C.8    Culbert, A.A.9    Brown, M.J.B.10    Smith, D.G.11    Reith, A.D.12
  • 20
    • 38149081185 scopus 로고    scopus 로고
    • note
    • 33P]ATP. After 40 min, the reaction was stopped by addition of 100 mM EDTA and 1.0 mM ATP, solution in 100 mM Hepes followed by a solution of streptavidin coated SPA beads (Amersham) in PBS to give a final concentration of 0.25 mg of beads per assay well. The plates were counted on a Packard TopCount NXT microplate counter.
  • 21
    • 38149131170 scopus 로고    scopus 로고
    • note
    • 50 values shown from repeat experiments are means (n = 3).
  • 22
    • 38149004212 scopus 로고    scopus 로고
    • note
    • Mouse TNF-α release assay; compound was administered orally to balb/c mice 30 min prior to LPS (0.1 mg/kg ip) challenge. Serum TNF-α levels were determined 90 min after LPS insult. Results represent means (n = 3).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.