2c1b

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[[Image:2c1b.gif|left|200px]]
[[Image:2c1b.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2c1b |SIZE=350|CAPTION= <scene name='initialview01'>2c1b</scene>, resolution 2.00&Aring;
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The line below this paragraph, containing "STRUCTURE_2c1b", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Cqp+Binding+Site+For+Chain+A'>AC1</scene>
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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=CQP:(4R,2S)-5&#39;-(4-(4-CHLOROBENZYLOXY)PYRROLIDIN-2-YLMETHANESULFONYL)ISOQUINOLINE'>CQP</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=
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-->
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|DOMAIN=
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{{STRUCTURE_2c1b| PDB=2c1b | 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=2c1b FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2c1b OCA], [http://www.ebi.ac.uk/pdbsum/2c1b PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2c1b RCSB]</span>
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}}
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'''STRUCTURE OF CAMP-DEPENDENT PROTEIN KINASE COMPLEXED WITH (4R,2S)-5'-(4-(4-CHLOROBENZYLOXY)PYRROLIDIN-2-YLMETHANESULFONYL)ISOQUINOLINE'''
'''STRUCTURE OF CAMP-DEPENDENT PROTEIN KINASE COMPLEXED WITH (4R,2S)-5'-(4-(4-CHLOROBENZYLOXY)PYRROLIDIN-2-YLMETHANESULFONYL)ISOQUINOLINE'''
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[[Category: Workman, P.]]
[[Category: Workman, P.]]
[[Category: Wyatt, P G.]]
[[Category: Wyatt, P G.]]
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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: complex (transferase/inhibitor)]]
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[[Category: Phosphorylation]]
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[[Category: phosphorylation]]
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[[Category: Protein kinase inhibitor]]
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[[Category: protein kinase inhibitor]]
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[[Category: Serine/threonine-protein kinase]]
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[[Category: serine/threonine-protein kinase]]
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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 Sat May 3 21:05:38 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:14:49 2008''
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Revision as of 18:05, 3 May 2008

Image:2c1b.gif

Template:STRUCTURE 2c1b

STRUCTURE OF CAMP-DEPENDENT PROTEIN KINASE COMPLEXED WITH (4R,2S)-5'-(4-(4-CHLOROBENZYLOXY)PYRROLIDIN-2-YLMETHANESULFONYL)ISOQUINOLINE


Overview

Structure-based drug design of novel isoquinoline-5-sulfonamide inhibitors of PKB as potential antitumour agents was investigated. Constrained pyrrolidine analogues that mimicked the bound conformation of linear prototypes were identified and investigated by co-crystal structure determinations with the related protein PKA. Detailed variation in the binding modes between inhibitors with similar overall conformations was observed. Potent PKB inhibitors from this series inhibited GSK3beta phosphorylation in cellular assays, consistent with inhibition of PKB kinase activity in cells.

About this Structure

2C1B is a Protein complex structure of sequences from Bos taurus and Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B., Collins I, Caldwell J, Fonseca T, Donald A, Bavetsias V, Hunter LJ, Garrett MD, Rowlands MG, Aherne GW, Davies TG, Berdini V, Woodhead SJ, Davis D, Seavers LC, Wyatt PG, Workman P, McDonald E, Bioorg Med Chem. 2006 Feb 15;14(4):1255-73. Epub 2005 Oct 24. PMID:16249095 Page seeded by OCA on Sat May 3 21:05:38 2008

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OCA

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