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Volumn 16, Issue 18, 2006, Pages 4728-4732

Synthesis and evaluation of thiazepines as interleukin-1β converting enzyme (ICE) inhibitors

Author keywords

Caspase 1; ICE; Interleukin 1 ; Peptidomimetic; Thiazepine

Indexed keywords

CASPASE 3; CASPASE 8; INTERLEUKIN 1BETA CONVERTING ENZYME INHIBITOR; PRALNACASAN; THIAZEPINE DERIVATIVE;

EID: 33746794165     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.07.016     Document Type: Article
Times cited : (13)

References (26)
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    • note
    • Partially presented at the 29th National Medicinal Chemistry Symposium, Madison, WI, June 2004. Ellis, C. D.; Oppong, K. A.; Laufersweiler, M. C.; O'Neil, S. V.; Soper, D. L.; Wang, Y.; Wos, J. A.; Fancher, A. N.; Lu, W.; Suchanek, M. K.; Wang, R. L; De, B. Poster # 110.
  • 2
    • 0027916179 scopus 로고
    • For a review on IL-1 biology, see:
    • For a review on IL-1 biology, see:. Dinarello C.A., and Wolff S.M. N. Eng. J. Med. 328 (1993) 106
    • (1993) N. Eng. J. Med. , vol.328 , pp. 106
    • Dinarello, C.A.1    Wolff, S.M.2
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    • Randall, J. C. R. Abstracts of Papers, 228th ACS National Meeting, Philadelphia, PA, August 2004, MEDI-200.
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    • Wang, Y.; O'Neil, S. V.; Wos, J. A.; Oppong, K. A.; Laufersweiler, M. C.; Soper, D. L.; Ellis, C. D.; Baize, M. W.; Bosch, G. K.; Fancher, A. N.; Lu, W.; Suchanek, M. K.; Wang, R. L.; Schwecke, W. P.; Cruze, C. A.; Buchalova, M.; Belkin, M.; De, B.; Demuth, T. P., Jr., 2006, manuscript in preparation.
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    • note
    • +.
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    • Robidoux, A. L. C; Wilson, J. D.; Dieterich, P.; Storer, N.; Leonardi, S. World Patent WO 00/10979, 2000.
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    • note
    • o is the initial velocity in the absence of inhibitor.
  • 25
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    • note
    • 6/ml in RPMI 1640 medium from Gibco BRL) was plated in 96-well plates, incubated with or without compounds (administered as solutions in DMSO, such that test concentrations ranged from 1 nM to 10 μM) for 15 min, and then stimulated with LPS (1 μg/ml) for 4 h. Cells were centrifuged and the conditioned media were collected to quantify the release of IL-1β by an ELISA measurement according to the manufacturer's instructions (R&D Systems, catalog number DLB50) or stored at -20 °C for future use.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.