2dq7: Difference between revisions

Revision as of 18:01, 21 February 2008

Crystal Structure of Fyn kinase domain complexed with staurosporine

OverviewOverview

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.

About this StructureAbout this Structure

2DQ7 is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Non-specific protein-tyrosine kinase, with EC number 2.7.10.2 Full crystallographic information is available from OCA.

ReferenceReference

Structure of human Fyn kinase domain complexed with staurosporine., Kinoshita T, Matsubara M, Ishiguro H, Okita K, Tada T, Biochem Biophys Res Commun. 2006 Aug 4;346(3):840-4. Epub 2006 Jun 13. PMID:16782058

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-[[Image:2dq7.gif|left|200px]]<br />
+[[Image:2dq7.gif|left|200px]]<br /><applet load="2dq7" size="350" color="white" frame="true" align="right" spinBox="true"
-<applet load="2dq7" size="450" color="white" frame="true" align="right" spinBox="true"
 caption="2dq7, resolution 2.8&Aring;" />
 '''Crystal Structure of Fyn kinase domain complexed with staurosporine'''<br />
 ==Overview==
-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.
+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.
 ==About this Structure==
-DQ7 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with STU as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2DQ7 OCA].
+DQ7 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=STU:'>STU</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Non-specific_protein-tyrosine_kinase Non-specific protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.2 2.7.10.2] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2DQ7 OCA].
 ==Reference==
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 [[Category: staurosporine]]
-''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 21:39:13 2007''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:01:24 2008''