2jdo: Difference between revisions

Revision as of 13:39, 30 October 2007

STRUCTURE OF PKB-BETA (AKT2) COMPLEXED WITH ISOQUINOLINE-5-SULFONIC ACID (2-(2-(4-CHLOROBENZYLOXY) ETHYLAMINO)ETHYL) AMIDE

OverviewOverview

Although the crystal structure of the anti-cancer target protein kinase B, (PKBbeta/Akt-2) has been useful in guiding inhibitor design, the closely, related kinase PKA has generally been used as a structural mimic due to, its facile crystallization with a range of ligands. The use of, PKB-inhibitor crystallography would bring important benefits, including a, more rigorous understanding of factors dictating PKA/PKB selectivity, and, the opportunity to validate the utility of PKA-based surrogates. We, present a "back-soaking" method for obtaining PKBbeta-ligand crystal, structures, and provide a structural comparison of inhibitor binding to, PKB, PKA, and PKA-PKB chimera. One inhibitor presented here exhibits no, PKB/PKA selectivity, and the compound adopts a similar binding mode in all, ... [(full description)]

About this StructureAbout this Structure

2JDO is a [Protein complex] structure of sequences from [Homo sapiens] with I5S and EDO as [ligands]. Active as [Non-specific serine/threonine protein kinase], with EC number [2.7.11.1]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].

ReferenceReference

A structural comparison of inhibitor binding to PKB, PKA and PKA-PKB chimera., Davies TG, Verdonk ML, Graham B, Saalau-Bethell S, Hamlett CC, McHardy T, Collins I, Garrett MD, Workman P, Woodhead SJ, Jhoti H, Barford D, J Mol Biol. 2007 Mar 30;367(3):882-94. Epub 2007 Jan 9. PMID:17275837

Page seeded by OCA on Tue Oct 30 12:44:12 2007

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA

@@ Line 8: / Line 8: @@
 ==About this Structure==
-JDO is a [[http://en.wikipedia.org/wiki/Protein_complex Protein complex]] structure of sequences from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with I5S and EDO as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[http://en.wikipedia.org/wiki/ ]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2JDO OCA]].
+JDO is a [[http://en.wikipedia.org/wiki/Protein_complex Protein complex]] structure of sequences from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with I5S and EDO as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[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]]. Structure known Active Site: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2JDO OCA]].
 ==Reference==
 A structural comparison of inhibitor binding to PKB, PKA and PKA-PKB chimera., Davies TG, Verdonk ML, Graham B, Saalau-Bethell S, Hamlett CC, McHardy T, Collins I, Garrett MD, Workman P, Woodhead SJ, Jhoti H, Barford D, J Mol Biol. 2007 Mar 30;367(3):882-94. Epub 2007 Jan 9. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17275837 17275837]
 [[Category: Homo sapiens]]
+[[Category: Non-specific serine/threonine protein kinase]]
 [[Category: Protein complex]]
 [[Category: Barford, D.]]
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 [[Category: wnt signaling pathway]]
-''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Oct 29 19:40:40 2007''
+''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 12:44:12 2007''