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Volumn 17, Issue 5, 2007, Pages 1296-1301

N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3

Author keywords

Inhibitor; JNK; JNK3; Kinase; MAPK; Selective

Indexed keywords

ADENOSINE TRIPHOSPHATE; MITOGEN ACTIVATED PROTEIN KINASE; MITOGEN ACTIVATED PROTEIN KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE 12; MITOGEN ACTIVATED PROTEIN KINASE P38; N (3 CYANO 4,5,6,7 TETRAHYDRO 1 BENZOTHIEN 2 YL)AMIDE; STRESS ACTIVATED PROTEIN KINASE INHIBITOR; SYNAPTOPHYSIN; UNCLASSIFIED DRUG;

EID: 33847000556     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.12.003     Document Type: Article
Times cited : (77)

References (28)
  • 13
    • 33847004856 scopus 로고    scopus 로고
    • note
    • 11 p38α inhibitory activity data were generated using conditions previously described, see: Barker, M. D.; Hamblin, J. N.; Jones, K. L.; Patel, V. K.; Swanson, S.; Walker, A. L. Int. Patent Appl. WO 05/073232.
  • 14
    • 0344177511 scopus 로고    scopus 로고
    • ERK2 kinase inhibitory activity was determined in a similar fashion to that described above for JNK3, using recombinant full length ERK2 expressed and purified as previously described, see: The ERK2 used for the work described in this paper was not activated before or during the assay
    • ERK2 kinase inhibitory activity was determined in a similar fashion to that described above for JNK3, using recombinant full length ERK2 expressed and purified as previously described, see:. McDonald O.B., Chen W.J., Ellis B., Hoffman C., Overton L., Rink M., Smith A., Marshall C.J., and Wood E.R. Anal. Biochem. 268 (1999) 318 The ERK2 used for the work described in this paper was not activated before or during the assay
    • (1999) Anal. Biochem. , vol.268 , pp. 318
    • McDonald, O.B.1    Chen, W.J.2    Ellis, B.3    Hoffman, C.4    Overton, L.5    Rink, M.6    Smith, A.7    Marshall, C.J.8    Wood, E.R.9
  • 15
    • 33846949470 scopus 로고    scopus 로고
    • note
    • 2 and 1 mM AMP-PNP. The crystals were grown at 10 °C, using the hanging drop vapour diffusion method, with a reservoir solution of 50 mM Tris/HCl, pH 7.2-7.6, 18-22% PEG3350 and 0.2 M KF and 1 μl + 1 μl hanging drops. JNK3t+MgAMP-PNP cocrystals were soaked at 20 °C in 50 mM Tris/HCl, pH 7.5, 20% PEG3350, and 0.2 M KF containing 0.8 mM inhibitor 5e for 4 days. The 8a complex was obtained in a similar way though crystals were soaked for 1 day in buffer (10 μL) containing 0.1 mg of solid 8a with 1 mM EDTA. Each crystal was cryoprotected by brief immersion into paratone-N (Hampton Research) prior to data collection. The PDB deposition codes for the 5e and 8a JNK3 complex crystal structures are 2O2U and 2O0U, respectively.
  • 28
    • 33846963281 scopus 로고    scopus 로고
    • note
    • 33P]ATP (45 μM). For further details, see: www.upstate.com.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.