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TitleHit to lead account of the discovery of a new class of inhibitors of Pim kinases and crystallographic studies revealing an unusual kinase binding mode.
Journal, issue, pagesJ. Med. Chem., Vol. 52, Page 1814-1827, Year 2009
Publish dateOct 29, 2008 (structure data deposition date)
AuthorsQian, K. / Wang, L. / Cywin, C.L. / Farmer, B.T. / Hickey, E. / Homon, C. / Jakes, S. / Kashem, M.A. / Lee, G. / Leonard, S. ...Qian, K. / Wang, L. / Cywin, C.L. / Farmer, B.T. / Hickey, E. / Homon, C. / Jakes, S. / Kashem, M.A. / Lee, G. / Leonard, S. / Li, J. / Magboo, R. / Mao, W. / Pack, E. / Peng, C. / Prokopowicz, A. / Welzel, M. / Wolak, J. / Morwick, T.
External linksJ. Med. Chem. / PubMed:19256503
MethodsX-ray diffraction
Resolution1.9 Å
Structure data

PDB-3f2a:
Crystal structure of human Pim-1 in complex with DAPPA
Method: X-RAY DIFFRACTION / Resolution: 1.9 Å

Chemicals

ChemComp-985:
(2E)-3-{3-[6-(4-methyl-1,4-diazepan-1-yl)pyrazin-2-yl]phenyl}prop-2-enoic acid

ChemComp-MG:
Unknown entry

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / potein kinase fold / Alternative initiation / ATP-binding / Cell membrane / Cytoplasm / Kinase / Manganese / Membrane / Metal-binding / Nucleotide-binding / Nucleus / Phosphoprotein / Polymorphism / Proto-oncogene / Serine/threonine-protein kinase

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