2hk5

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[[Image:2hk5.jpg|left|200px]]
[[Image:2hk5.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2hk5 |SIZE=350|CAPTION= <scene name='initialview01'>2hk5</scene>, resolution 2.0&Aring;
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The line below this paragraph, containing "STRUCTURE_2hk5", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=1BM:3-{[2-(1H-BENZIMIDAZOL-1-YL)-6-{[2-(DIETHYLAMINO)ETHYL]AMINO}PYRIMIDIN-4-YL]AMINO}-4-METHYLPHENOL'>1BM</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <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>
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or leave the SCENE parameter empty for the default display.
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|GENE= HCK ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2hk5| PDB=2hk5 | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2hk5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2hk5 OCA], [http://www.ebi.ac.uk/pdbsum/2hk5 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2hk5 RCSB]</span>
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}}
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'''Hck Kinase in Complex with Lck targetted Inhibitor PG-1009247'''
'''Hck Kinase in Complex with Lck targetted Inhibitor PG-1009247'''
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[[Category: Sabat, M P.]]
[[Category: Sabat, M P.]]
[[Category: Walter, R L.]]
[[Category: Walter, R L.]]
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[[Category: hck]]
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[[Category: Hck]]
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[[Category: kinase domain]]
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[[Category: Kinase domain]]
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[[Category: src-family]]
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[[Category: Src-family]]
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[[Category: transferase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 06:23:13 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:31:29 2008''
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Revision as of 03:23, 4 May 2008

Template:STRUCTURE 2hk5

Hck Kinase in Complex with Lck targetted Inhibitor PG-1009247


Overview

This communication details the synthesis, biological activity, and binding mode of a novel class of 2-benzimidazole substituted pyrimidines. The most potent analogs disclosed showed low nanomolar activity for the inhibition of Lck kinase and a representative analog was co-crystallized with Hck (a structurally related member of the Src family kinases).

About this Structure

2HK5 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

The development of 2-benzimidazole substituted pyrimidine based inhibitors of lymphocyte specific kinase (Lck)., Sabat M, VanRens JC, Laufersweiler MJ, Brugel TA, Maier J, Golebiowski A, De B, Easwaran V, Hsieh LC, Walter RL, Mekel MJ, Evdokimov A, Janusz MJ, Bioorg Med Chem Lett. 2006 Dec 1;16(23):5973-7. Epub 2006 Sep 25. PMID:16997556 Page seeded by OCA on Sun May 4 06:23:13 2008

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