2c0t

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[[Image:2c0t.gif|left|200px]]<br /><applet load="2c0t" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2c0t.gif|left|200px]]
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caption="2c0t, resolution 2.15&Aring;" />
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'''SRC FAMILY KINASE HCK WITH BOUND INHIBITOR A-641359'''<br />
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{{Structure
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|PDB= 2c0t |SIZE=350|CAPTION= <scene name='initialview01'>2c0t</scene>, resolution 2.15&Aring;
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|SITE= <scene name='pdbsite=AC1:Ca+Binding+Site+For+Chain+B'>AC1</scene>
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|LIGAND= <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene> and <scene name='pdbligand=L3G:N-(4-{4-AMINO-1-[1-(TETRAHYDRO-2H-PYRAN-4-YL)PIPERIDIN-4-YL]-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL}-2-METHOXYPHENYL)-1-METHYL-1H-INDOLE-2-CARBOXAMIDE'>L3G</scene>
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|ACTIVITY= [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.10.1_and_2.7.10.2 Transferred entry: 2.7.10.1 and 2.7.10.2], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.112 2.7.1.112]
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|GENE=
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}}
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'''SRC FAMILY KINASE HCK WITH BOUND INHIBITOR A-641359'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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2C0T 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=CA:'>CA</scene> and <scene name='pdbligand=L3G:'>L3G</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.10.1_and_2.7.10.2 Transferred entry: 2.7.10.1 and 2.7.10.2], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.112 2.7.1.112] Known structural/functional Site: <scene name='pdbsite=AC1:Ca+Binding+Site+For+Chain+B'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2C0T OCA].
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2C0T is a [[Single protein]] structure of 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=2C0T OCA].
==Reference==
==Reference==
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Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection., Burchat A, Borhani DW, Calderwood DJ, Hirst GC, Li B, Stachlewitz RF, Bioorg Med Chem Lett. 2006 Jan 1;16(1):118-22. Epub 2005 Oct 10. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16216497 16216497]
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Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection., Burchat A, Borhani DW, Calderwood DJ, Hirst GC, Li B, Stachlewitz RF, Bioorg Med Chem Lett. 2006 Jan 1;16(1):118-22. Epub 2005 Oct 10. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16216497 16216497]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: tyrosine-protein kinase]]
[[Category: tyrosine-protein kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:43:39 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 16:09:24 2008''

Revision as of 14:09, 20 March 2008


PDB ID 2c0t

Drag the structure with the mouse to rotate
, resolution 2.15Å
Sites:
Ligands: and
Activity: Transferred entry: 2.7.10.1 and 2.7.10.2, with EC number 2.7.1.112
Coordinates: save as pdb, mmCIF, xml



SRC FAMILY KINASE HCK WITH BOUND INHIBITOR A-641359


Overview

We describe the identification, SAR, and pharmacology of the src-family selective lck inhibitor A-770041 that prolongs the survival of major histocompatibility mismatched allografts in models of solid organ transplant rejection for greater than 65 days.

About this Structure

2C0T is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection., Burchat A, Borhani DW, Calderwood DJ, Hirst GC, Li B, Stachlewitz RF, Bioorg Med Chem Lett. 2006 Jan 1;16(1):118-22. Epub 2005 Oct 10. PMID:16216497

Page seeded by OCA on Thu Mar 20 16:09:24 2008

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