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Volumn 16, Issue 9, 2006, Pages 2337-2340

The design and synthesis of human branched-chain amino acid aminotransferase inhibitors for treatment of neurodegenerative diseases

Author keywords

[No Author keywords available]

Indexed keywords

AMINOTRANSFERASE INHIBITOR; BRANCHED CHAIN AMINO ACID AMINOTRANSFERASE; GLUTAMIC ACID;

EID: 33644986624     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.07.058     Document Type: Article
Times cited : (25)

References (18)
  • 7
    • 33644972043 scopus 로고    scopus 로고
    • note
    • 4b The amount of GDH was determined for each preparation to ensure the saturating level for the assay;
  • 9
    • 33644984286 scopus 로고    scopus 로고
    • note
    • Inhibitors were solubilized in DMSO at a primary concentration of 10 mM and then diluted to give a final concentration between 0.3 and 100 μM. The assay is done in a 96-well plate. Total reaction volume of 100 μl consisted of 58 μl reaction mixture with 2μl of specified inhibitor and 38 μl water. The reaction was started with 2 μl BCAT enzyme. The 96-well reaction plate was incubated for 30 min at 37°C. The reaction was stopped with 100μl of 2% acetic acid (1% Final) and analyzed for glutamate with LC/MS/MS.
  • 10
    • 33644987845 scopus 로고    scopus 로고
    • note
    • 45Ca uptake was determined thirty minutes following the addition of LPDC. Cultures were washed trice with 500 ml HBSS and then dissolved with lysate buffer. Individual lysates were combined with 10 ml scintillation cocktail and counted for emissions using a Tricarb 2900TR Packard Liquid Scintillation Analyzer;
  • 13
    • 33644969344 scopus 로고    scopus 로고
    • note
    • 11 For evaluation of brain damage, sections were examined with a light microscope for detecting positive staining black areas that implied areas of neuronal death. Total number of sections with the positive findings from each group was finally compared with other groups (Newman-Keuls).
  • 14
    • 33644973748 scopus 로고    scopus 로고
    • note
    • 6) δ 7.44 (dd, 1H, J = 9.04 and 2.20 Hz), 7.53 (s, 1H), 7.63 (d, 1H, J = 8.79 Hz), 7.75-7.82 (m, 2H), 7.84 (d, 1H, J = 1.95 Hz), 7.93 (dd, 1H, J = 2.2 and 9.03 Hz), 8.13 (dd, 1H, J = 2.44 and 6.59 Hz), 10.19 (s, 1H), and 11.06 (s, 1H);
  • 16
    • 33644968247 scopus 로고    scopus 로고
    • Tripos Associates, St. Louis, MO;
    • Tripos Associates, St. Louis, MO;
  • 17
    • 33644989206 scopus 로고    scopus 로고
    • note
    • Coordinates have been deposited with the RCSB Protein Data Bank with the ID cods 2ABJ.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.