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2h9v

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[[Image:2h9v.gif|left|200px]]
[[Image:2h9v.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2h9v |SIZE=350|CAPTION= <scene name='initialview01'>2h9v</scene>, resolution 3.100&Aring;
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The line below this paragraph, containing "STRUCTURE_2h9v", 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=Y27:(R)-TRANS-4-(1-AMINOETHYL)-N-(4-PYRIDYL)+CYCLOHEXANECARBOXAMIDE'>Y27</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_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_2h9v| PDB=2h9v | SCENE= }}
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|RELATEDENTRY=[[2f2u|2F2U]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2h9v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2h9v OCA], [http://www.ebi.ac.uk/pdbsum/2h9v PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2h9v RCSB]</span>
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}}
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'''Structural basis for induced-fit binding of Rho-kinase to the inhibitor Y27632'''
'''Structural basis for induced-fit binding of Rho-kinase to the inhibitor Y27632'''
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[[Category: Miwa, Y.]]
[[Category: Miwa, Y.]]
[[Category: Yamaguchi, H.]]
[[Category: Yamaguchi, H.]]
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[[Category: protein kinase-inhibitor complex]]
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[[Category: Protein kinase-inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 06:02:06 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:27:36 2008''
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Revision as of 03:02, 4 May 2008

Image:2h9v.gif

Template:STRUCTURE 2h9v

Structural basis for induced-fit binding of Rho-kinase to the inhibitor Y27632


Overview

Rho-kinase is a main player in the regulation of cytoskeletal events and a promising drug target in the treatment of both vascular and neurological disorders. Here we report the crystal structure of the Rho-kinase catalytic domain in complex with the specific inhibitor Y-27632. Comparison with the structure of PKA bound to this inhibitor revealed a potential induced-fit binding mode that can be accommodated by the phosphate binding loop. This binding mode resembles to that observed in the Rho-kinase-fasudil complex. A structural database search indicated that a pocket underneath the phosphate-binding loop is present that favors binding to a small aromatic ring. Introduction of such a ring group might spawn a new modification scheme of pre-existing protein kinase inhibitors for improved binding capability.

About this Structure

2H9V is a Single protein structure of sequence from Bos taurus. Full crystallographic information is available from OCA.

Reference

Structural basis for induced-fit binding of Rho-kinase to the inhibitor Y-27632., Yamaguchi H, Miwa Y, Kasa M, Kitano K, Amano M, Kaibuchi K, Hakoshima T, J Biochem. 2006 Sep;140(3):305-11. Epub 2006 Aug 4. PMID:16891330 Page seeded by OCA on Sun May 4 06:02:06 2008

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