1xh4

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[[Image:1xh4.gif|left|200px]]
[[Image:1xh4.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1xh4 |SIZE=350|CAPTION= <scene name='initialview01'>1xh4</scene>, resolution 2.45&Aring;
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The line below this paragraph, containing "STRUCTURE_1xh4", 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=R69:N-[4-({4-[5-(DIMETHYLAMINO)-2-HYDROXYBENZOYL]BENZOYL}AMINO)AZEPAN-3-YL]ISONICOTINAMIDE'>R69</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_1xh4| PDB=1xh4 | SCENE= }}
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|RELATEDENTRY=[[1svh|1SVH]], [[1sve|1SVE]], [[1svg|1SVG]], [[1veb|1VEB]], [[1xh5|1XH5]], [[1xh6|1XH6]], [[1xh7|1XH7]], [[1xh8|1XH8]], [[1xh9|1XH9]], [[1xha|1XHA]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1xh4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1xh4 OCA], [http://www.ebi.ac.uk/pdbsum/1xh4 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1xh4 RCSB]</span>
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}}
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'''Crystal Structures of Protein Kinase B Selective Inhibitors in Complex with Protein Kinase A and Mutants'''
'''Crystal Structures of Protein Kinase B Selective Inhibitors in Complex with Protein Kinase A and Mutants'''
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[[Category: Thomas, U.]]
[[Category: Thomas, U.]]
[[Category: Werner, G.]]
[[Category: Werner, G.]]
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[[Category: balanol derivative]]
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[[Category: Balanol derivative]]
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[[Category: kinase-inhibitor-complex]]
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[[Category: Kinase-inhibitor-complex]]
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[[Category: pka]]
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[[Category: Pka]]
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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 15:01:20 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:49:31 2008''
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Revision as of 12:01, 3 May 2008

Image:1xh4.gif

Template:STRUCTURE 1xh4

Crystal Structures of Protein Kinase B Selective Inhibitors in Complex with Protein Kinase A and Mutants


Overview

Protein kinase B (PKB)-selective inhibitors were designed, synthesized, and cocrystallized using the AGC kinase family protein kinase A (PKA, often called cAMP-dependent protein kinase); PKA has been used as a surrogate for other members of this family and indeed for protein kinases in general. The high homology between PKA and PKB includes very similar ATP binding sites and hence similar binding pockets for inhibitors, with only few amino acids that differ between the two kinases. A series of these sites were mutated in PKA in order to improve the surrogate model for a design of PKB-selective inhibitors. Namely, the PKA to PKB exchanges F187L and Q84E enable the design of the selective inhibitors described herein which mimic ATP but extend further into a site not occupied by ATP. In this pocket, selectivity over PKA can be achieved by the introduction of bulkier substituents. Analysis of the cocrystal structures and binding studies were performed to rationalize the selectivity and improve the design.

About this Structure

1XH4 is a Protein complex structure of sequences from Bos taurus. Full crystallographic information is available from OCA.

Reference

Design and crystal structures of protein kinase B-selective inhibitors in complex with protein kinase A and mutants., Breitenlechner CB, Friebe WG, Brunet E, Werner G, Graul K, Thomas U, Kunkele KP, Schafer W, Gassel M, Bossemeyer D, Huber R, Engh RA, Masjost B, J Med Chem. 2005 Jan 13;48(1):163-70. PMID:15634010 Page seeded by OCA on Sat May 3 15:01:20 2008

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OCA

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