2c1b

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[[Image:2c1b.gif|left|200px]]<br />
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[[Image:2c1b.gif|left|200px]]<br /><applet load="2c1b" size="450" color="white" frame="true" align="right" spinBox="true"
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<applet load="2c1b" size="450" color="white" frame="true" align="right" spinBox="true"
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caption="2c1b, resolution 2.00&Aring;" />
caption="2c1b, resolution 2.00&Aring;" />
'''STRUCTURE OF CAMP-DEPENDENT PROTEIN KINASE COMPLEXED WITH (4R,2S)-5'-(4-(4-CHLOROBENZYLOXY)PYRROLIDIN-2-YLMETHANESULFONYL)ISOQUINOLINE'''<br />
'''STRUCTURE OF CAMP-DEPENDENT PROTEIN KINASE COMPLEXED WITH (4R,2S)-5'-(4-(4-CHLOROBENZYLOXY)PYRROLIDIN-2-YLMETHANESULFONYL)ISOQUINOLINE'''<br />
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==About this Structure==
==About this Structure==
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2C1B is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] and [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with CQP as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37] Structure known Active Site: AC1. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2C1B OCA].
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2C1B is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] and [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with CQP as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37] Known structural/functional Site: <scene name='pdbsite=AC1:Cqp Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2C1B OCA].
==Reference==
==Reference==
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[[Category: transferase]]
[[Category: transferase]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 21:09:30 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Dec 18 19:05:49 2007''

Revision as of 16:56, 18 December 2007

Image:2c1b.gif

2c1b, resolution 2.00Å

Drag the structure with the mouse to rotate

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 with CQP as ligand. Active as Transferred entry: 2.7.11.1, with EC number 2.7.1.37 Known structural/functional Site: . 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

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