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1q8u

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[[Image:1q8u.jpg|left|200px]]
[[Image:1q8u.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1q8u |SIZE=350|CAPTION= <scene name='initialview01'>1q8u</scene>, resolution 1.90&Aring;
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The line below this paragraph, containing "STRUCTURE_1q8u", 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=H52:(S)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLINE)SULFONYL]-HOMOPIPERAZINE'>H52</scene>, <scene name='pdbligand=MG8:N-OCTANOYL-N-METHYLGLUCAMINE'>MG8</scene>, <scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</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= PRKACA ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 Bos taurus])
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-->
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|DOMAIN=
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{{STRUCTURE_1q8u| PDB=1q8u | SCENE= }}
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|RELATEDENTRY=[[1q8t|1Q8T]], [[1q8w|1Q8W]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1q8u FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1q8u OCA], [http://www.ebi.ac.uk/pdbsum/1q8u PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1q8u RCSB]</span>
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}}
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'''The Catalytic Subunit of cAMP-dependent Protein Kinase in Complex with Rho-kinase Inhibitor H-1152P'''
'''The Catalytic Subunit of cAMP-dependent Protein Kinase in Complex with Rho-kinase Inhibitor H-1152P'''
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[[Category: Huber, R.]]
[[Category: Huber, R.]]
[[Category: Kinzel, V.]]
[[Category: Kinzel, V.]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: camp]]
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[[Category: Camp]]
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[[Category: kinase-inhibitor-complex]]
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[[Category: Kinase-inhibitor-complex]]
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[[Category: phosphorylation]]
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[[Category: Phosphorylation]]
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[[Category: phosphotransferase/inhibitor]]
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[[Category: Phosphotransferase/inhibitor]]
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[[Category: pka]]
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[[Category: Pka]]
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[[Category: rho-kinase]]
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[[Category: Rho-kinase]]
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[[Category: serine/threonine-protein kinase]]
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[[Category: Serine/threonine-protein kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 06:00:40 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:10:23 2008''
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Revision as of 03:00, 3 May 2008

Image:1q8u.jpg

Template:STRUCTURE 1q8u

The Catalytic Subunit of cAMP-dependent Protein Kinase in Complex with Rho-kinase Inhibitor H-1152P


Overview

Protein kinases require strict inactivation to prevent spurious cellular signaling; overactivity can cause cancer or other diseases and necessitates selective inhibition for therapy. Rho-kinase is involved in such processes as tumor invasion, cell adhesion, smooth muscle contraction, and formation of focal adhesion fibers, as revealed using inhibitor Y-27632. Another Rho-kinase inhibitor, HA-1077 or Fasudil, is currently used in the treatment of cerebral vasospasm; the related nanomolar inhibitor H-1152P improves on its selectivity and potency. We have determined the crystal structures of HA-1077, H-1152P, and Y-27632 in complexes with protein kinase A (PKA) as a surrogate kinase to analyze Rho-kinase inhibitor binding properties. Features conserved between PKA and Rho-kinase are involved in the key binding interactions, while a combination of residues at the ATP binding pocket that are unique to Rho-kinase may explain the inhibitors' Rho-kinase selectivity. Further, a second H-1152P binding site potentially points toward PKA regulatory domain interaction modulators.

About this Structure

1Q8U is a Protein complex structure of sequences from Bos taurus. Full crystallographic information is available from OCA.

Reference

Protein kinase A in complex with Rho-kinase inhibitors Y-27632, Fasudil, and H-1152P: structural basis of selectivity., Breitenlechner C, Gassel M, Hidaka H, Kinzel V, Huber R, Engh RA, Bossemeyer D, Structure. 2003 Dec;11(12):1595-607. PMID:14656443 Page seeded by OCA on Sat May 3 06:00:40 2008

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