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Volumn 15, Issue 9, 2005, Pages 2285-2289

The development of monocyclic pyrazolone based cytokine synthesis inhibitors

Author keywords

Cytokine synthesis inhibitors; p38 kinase

Indexed keywords

IODOACETIC ACID; LIPOPOLYSACCHARIDE; PYRAZOLONE DERIVATIVE; TUMOR NECROSIS FACTOR ALPHA;

EID: 20244384146     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.03.007     Document Type: Article
Times cited : (27)

References (17)
  • 1
    • 0035226687 scopus 로고    scopus 로고
    • P38 MAP Kinase: Molecular Target for the Inhibition of Pro-inflammatory Cytokines
    • F.D. King A.W. Oxford Elsevier Amsterdam
    • For a recent review, see: J.L. Adams, A.M. Badger, S. Kumar, and J.C. Lee p38 MAP Kinase: Molecular Target for the Inhibition of Pro-inflammatory Cytokines F.D. King A.W. Oxford Progress in Medicinal Chemistry 38 2001 Elsevier Amsterdam 1 60
    • (2001) Progress in Medicinal Chemistry , vol.38 , pp. 1-60
    • Adams, J.L.1    Badger, A.M.2    Kumar, S.3    Lee, J.C.4
  • 11
    • 85030797508 scopus 로고    scopus 로고
    • note
    • 15 (Promega Co., Madison, WI). Standard deviation for THP-1 cellular assays were typically ±30% of the mean or less
  • 12
  • 13
    • 85030794441 scopus 로고    scopus 로고
    • The mutated p38α herein described is an inactivated, double mutant (S180A, Y182F) of murine p38α. For more details see Ref. 7. The crystal structure of compound 15d bound to mutated p38α-kinase has been deposited in the Protein Data Bank with RCSB/PDB information is as follows: PDB Code: 1YWR; RCSB code: RCSB032009
    • The mutated p38α herein described is an inactivated, double mutant (S180A, Y182F) of murine p38α. For more details see Ref. 7. The crystal structure of compound 15d bound to mutated p38α-kinase has been deposited in the Protein Data Bank with RCSB/PDB information is as follows: PDB Code: 1YWR; RCSB code: RCSB032009
  • 16
    • 85030793820 scopus 로고    scopus 로고
    • note
    • Sprague-Dawley male rats (200-225 g) from Harlan (Oregon, WI) under anesthesia were injected in the patellar ligament region of the left leg (flexed 90°at the knee) with 20 μL of a 10 mg/mL concentration of monosodium iodoacetate (IA) (Aldrich Chemical, Milwaukee, WI). Animals (groups of 15) were dosed for 7 days BID (∼every 12 h) with the potential inhibitor (25 mg/kg) or vehicle (2.5 mL/kg). Animals were sacrificed on day 22 and the left joint was disarticulated and fixed in 10% formalin for 24-48 h prior to capturing the image. An image of the tibial cartilage surface was captured using an Optimas (Optimas, Media Cybernetics LP, Silver Springs, MA) image analysis system. Three independent observers assessed the damage in a blinded manner using a scale of 0-4 of increasing severity (0 = normal; 4 = maximum severity)


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.