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==Crystal structure of spleen tyrosine kinase complexed with an adamantylpyrazine inhibitor==
<StructureSection load='4dfn' size='340' side='right' caption='[[4dfn]], [[Resolution|resolution]] 2.48&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[4dfn]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4DFN OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4DFN FirstGlance]. <br>
</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0K1:3-AMINO-6-[3-(1-METHYL-1H-PYRAZOL-4-YL)PHENYL]-N-[(1R,2R,3S,5S,7S)-5-HYDROXYADAMANTAN-2-YL]PYRAZINE-2-CARBOXAMIDE'>0K1</scene><br>
<tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4dfl|4dfl]]</td></tr>
<tr><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">SYK ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>
<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[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] </span></td></tr>
<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4dfn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4dfn OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4dfn RCSB], [http://www.ebi.ac.uk/pdbsum/4dfn PDBsum]</span></td></tr>
<table>
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
A series of aminopyrazines as inhibitors of Syk kinase activity and showing inhibition of LAD2 cells degranulation is described. Optimization of the carboxamide motif with aminomethylpiperidines provided high potency inhibiting Syk but low cellular activity. Amides of cis and trans adamantanol showed good inhibitory activity against Syk as well as remarkable activity in LAD2 cells degranulation assay.


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Pyrazine-based Syk kinase inhibitors.,Forns P, Esteve C, Taboada L, Alonso JA, Orellana A, Maldonado M, Carreno C, Ramis I, Lopez M, Miralpeix M, Vidal B Bioorg Med Chem Lett. 2012 Apr 15;22(8):2784-8. Epub 2012 Mar 2. PMID:22425453<ref>PMID:22425453</ref>
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{{STRUCTURE_4dfn|  PDB=4dfn  |  SCENE=  }}


===Crystal structure of spleen tyrosine kinase complexed with an adamantylpyrazine inhibitor===
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>


 
==See Also==
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*[[Tyrosine kinase|Tyrosine kinase]]
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== References ==
(as it appears on PubMed at http://www.pubmed.gov), where 22425453 is the PubMed ID number.
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{{ABSTRACT_PUBMED_22425453}}
</StructureSection>
 
==About this Structure==
[[4dfn]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4DFN OCA].
 
==Reference==
<ref group="xtra">PMID:022425453</ref><references group="xtra"/>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Non-specific protein-tyrosine kinase]]
[[Category: Non-specific protein-tyrosine kinase]]

Revision as of 10:51, 5 June 2014

Crystal structure of spleen tyrosine kinase complexed with an adamantylpyrazine inhibitorCrystal structure of spleen tyrosine kinase complexed with an adamantylpyrazine inhibitor

Structural highlights

4dfn is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:
Related:4dfl
Gene:SYK (Homo sapiens)
Activity:Non-specific protein-tyrosine kinase, with EC number 2.7.10.2
Resources:FirstGlance, OCA, RCSB, PDBsum

Publication Abstract from PubMed

A series of aminopyrazines as inhibitors of Syk kinase activity and showing inhibition of LAD2 cells degranulation is described. Optimization of the carboxamide motif with aminomethylpiperidines provided high potency inhibiting Syk but low cellular activity. Amides of cis and trans adamantanol showed good inhibitory activity against Syk as well as remarkable activity in LAD2 cells degranulation assay.

Pyrazine-based Syk kinase inhibitors.,Forns P, Esteve C, Taboada L, Alonso JA, Orellana A, Maldonado M, Carreno C, Ramis I, Lopez M, Miralpeix M, Vidal B Bioorg Med Chem Lett. 2012 Apr 15;22(8):2784-8. Epub 2012 Mar 2. PMID:22425453[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

See Also

References

  1. ↑ Forns P, Esteve C, Taboada L, Alonso JA, Orellana A, Maldonado M, Carreno C, Ramis I, Lopez M, Miralpeix M, Vidal B. Pyrazine-based Syk kinase inhibitors. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2784-8. Epub 2012 Mar 2. PMID:22425453 doi:10.1016/j.bmcl.2012.02.087

4dfn, resolution 2.48Å

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