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Volumn 16, Issue 21, 2006, Pages 5659-5663

Design and synthesis of novel N-sulfonyl-2-indole carboxamides as potent PPAR-γ binding agents with potential application to the treatment of osteoporosis

Author keywords

Alkaline phosphatase assay; N Sulfonyl 2 indole carboxamides; Osteoporosis; PPAR

Indexed keywords

AMIDE; BINDING PROTEIN; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA;

EID: 33748873447     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.08.003     Document Type: Article
Times cited : (47)

References (36)
  • 19
    • 33748865283 scopus 로고    scopus 로고
    • Stolle, A.; Dumas, J. P.; Carley, W.; Coish, P. D. G.; Magnuson, S. R.; Wang, Y.; Nagarathnam, D.; Lowe, D. B.; Sun, N.; Bullock, W. H.; Campbell, A.-M.; Qi, N.; Baryza, J. L.; Cook, J. H. PCT Int. Appl., 2002 233pp.
  • 22
    • 33748880938 scopus 로고    scopus 로고
    • note
    • 1H NMR and high-resolution MS and found to be in agreement with their structures.
  • 24
    • 33748882479 scopus 로고    scopus 로고
    • note
    • +.
  • 25
    • 33748873558 scopus 로고    scopus 로고
    • note
    • d = 9 nM). The PPAR-γ LBD/Fluormone complex yielded a high fluorescence polarization value (mP). Competitor compound was added to the complex, displacing Fluormone, yielding a lower fluorescence polarization value. Compounds that do not compete for PPAR-γ LBD binding will not reduce the fluorescence polarization value.
  • 27
    • 33748869009 scopus 로고    scopus 로고
    • 6-PPAR-γ, 1 mM SRC-1 peptide fragment) was added to two microliters of well solution (2% Peg400, 1.6 M ammonium sulfate, and 100 mM Mes 6.5) and suspended over 1 mL of well solution in a hanging drop crystallization setup. The X-ray coordinates have been deposited with the Protein Data Bank, www.rcsb.org, as entries 2HFP (PPAR-γ/2a). Resolution for reported structures 2.0 Å.
  • 36
    • 33748880768 scopus 로고    scopus 로고
    • note
    • 2 (adjust to pH 10.5) was added to each well and the cells were incubated at room temperature for 20 min. Absorbance was read at 405 nm on a Molecular Devices SPECTRAmax PLUS 384 plate reader. The enzyme activity was expressed as pNP nmols/min/million cells.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.