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Volumn 20, Issue 1, 2010, Pages 330-333

2,4-Diaminopyrimidine MK2 inhibitors. Part I: Observation of an unexpected inhibitor binding mode

Author keywords

Diaminopyrimidine; MAPKAP K2; MK2; TNF

Indexed keywords

2,4 DIAMINOPYRIMIDINE DERIVATIVE; MITOGEN ACTIVATED PROTEIN KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE 2 INHIBITOR; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; UNCLASSIFIED DRUG;

EID: 72049116018     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.10.102     Document Type: Article
Times cited : (23)

References (26)
  • 10
    • 72049121706 scopus 로고    scopus 로고
    • Harris, C. M.; Ericsson, A. M.; Argiriadi, M. A.; Barberis, C.; Borhani, D. W.; Burchat, A.; Calderwood, D. J.; Cunha, G. A.; Dixon, R. W.; Frank, K. E.; Johnson, E. F.; Kamens, J.; Kwak, S.; Li, B.; Mullen, K. D.; Perron, D. C.; Wang, L.; Wishart, N.; Wu, X.; Zhang, X.; Zmetra, T. R.; Talanian, R. V. Bioorg. Med. Chem. Lett. (2009), doi:10.1016/jbmcl.2009.10.103.
    • Harris, C. M.; Ericsson, A. M.; Argiriadi, M. A.; Barberis, C.; Borhani, D. W.; Burchat, A.; Calderwood, D. J.; Cunha, G. A.; Dixon, R. W.; Frank, K. E.; Johnson, E. F.; Kamens, J.; Kwak, S.; Li, B.; Mullen, K. D.; Perron, D. C.; Wang, L.; Wishart, N.; Wu, X.; Zhang, X.; Zmetra, T. R.; Talanian, R. V. Bioorg. Med. Chem. Lett. (2009), doi:10.1016/jbmcl.2009.10.103.
  • 11
    • 72049087552 scopus 로고    scopus 로고
    • note
    • To measure the effect of p38 activation, nonphosphorylated MK2 samples were assayed with and without 2 ng active p38α (upstate, no 14-251). Separate experiments demonstrated that p38α does not activate the MK2 assay peptide substrate (not shown).
  • 25
    • 72049084593 scopus 로고    scopus 로고
    • note
    • free 29.7 and 26.5, respectively. The coordinates for the crystal structures of MK2/2 and MK2/3 are deposited in the Protein Data Bank with IDs 3KC3 and 3KA0, respectively. Full details of crystal data collection, structure determination and a table of structure statistics are in Supplementary data.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.