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Volumn 23, Issue 3, 2013, Pages 791-796

Discovery of liver-targeted inhibitors of stearoyl-CoA desaturase (SCD1)

Author keywords

Liver targeted inhibitors; Saturated fatty acids; Spirocyclic oxazepine; Stearoyl coenzyme A desaturase 1; Unsaturated fatty acids

Indexed keywords

ACYL COENZYME A DESATURASE 1; GLYCINAMIDE; OXAZEPINE DERIVATIVE; OXYGENASE INHIBITOR; PIPERIDINE; THIAZOLE;

EID: 84872358339     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.11.075     Document Type: Article
Times cited : (17)

References (26)
  • 23
    • 72249113143 scopus 로고    scopus 로고
    • S. Leger, W.C. Black, D. Deschenes, S. Dolman, J.P. Falgueyret, M. Gagnon, S. Guiral, Z. Huang, J. Guay, Y. Leblanc, C.S. Li, F. Masse, R. Oballa, and L. Zhang Bioorg. Med. Chem. Lett. 20 2010 499 detailed procedure as following: in 100 μl of 100 mM Tris HCl, pH 7.3/2 mM NADH/20 μM stearoyl-CoA containing 0.75 μCi [9,10-3H-stearoyl] stearoyl-CoA per well. After a 15-min incubation at room temperature, plates were transferred to ice and 10 μl of 20% trichloroacetic acid was added to each well. After 5 min on ice, a 90-μl volume from each well was transferred to a Millipore Multiscreen HTS 96-well filtration plate, the wells of which contained 125 μl of 10% activated charcoal to which vacuum had been previously applied to remove excess liquid and a plastic seal then applied to the bottom. Plates were shaken 15 min and the contents were then filtered into a 96-well collection plate. A 50-μl volume of filtrate was counted in 150 μl of MicroScint 40 in a TopCount scintillation counter. Stock solutions of compounds, 10 mM in DMSO, were diluted in DMSO for a final assay concentration of 2% DMSO. Percent inhibition was determined as (total-sample)/(total-blank)(100); total activity was determined in the presence of 2% DMSO and blank in the presence of 10-4 M concentration of a standard inhibitor in 2% DMSO. The inhibition constant was determined with the Prism non-linear, least-squares, curve-fitting program
    • (2010) Bioorg. Med. Chem. Lett. , vol.20 , pp. 499
    • Leger, S.1    Black, W.C.2    Deschenes, D.3    Dolman, S.4    Falgueyret, J.P.5    Gagnon, M.6    Guiral, S.7    Huang, Z.8    Guay, J.9    Leblanc, Y.10    Li, C.S.11    Masse, F.12    Oballa, R.13    Zhang, L.14


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.