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PDBsum entry 2dq7
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References listed in PDB file
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Key reference
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Title
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Structure of human fyn kinase domain complexed with staurosporine.
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Authors
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T.Kinoshita,
M.Matsubara,
H.Ishiguro,
K.Okita,
T.Tada.
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Ref.
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Biochem Biophys Res Commun, 2006,
346,
840-844.
[DOI no: ]
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PubMed id
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Abstract
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The tyrosine kinase Fyn is a member of the Src kinase family. Besides the role
of Fyn in T cell signal transduction in concert with Lck, its excess activity in
the brain is involved with conditions such as Alzheimer's and Parkinson's
diseases. Therefore, inhibition of Fyn kinase may help counteract these nervous
system disorders. Here, we solved the crystal structure of the human Fyn kinase
domain complexed with staurosporine, a potent kinase inhibitor, at 2.8 A
resolution. Staurosporine binds to the ATP-binding site of Fyn in a similar
manner as in the Lck- and Csk-complexes. The small structural differences in the
staurosporine-binding and/or -unbinding region among the three kinase domains
may help obtaining the selective inhibitors against the respective kinases.
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