2jdo: Difference between revisions

From Proteopedia
Jump to navigation Jump to search
No edit summary
No edit summary
Line 1: Line 1:
[[Image:2jdo.gif|left|200px]]
{{Seed}}
[[Image:2jdo.png|left|200px]]


<!--
<!--
Line 9: Line 10:
{{STRUCTURE_2jdo|  PDB=2jdo  |  SCENE=  }}  
{{STRUCTURE_2jdo|  PDB=2jdo  |  SCENE=  }}  


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




==Overview==
<!--  
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 three systems. By contrast, the PKB-selective inhibitor A-443654 adopts a conformation in PKB and PKA-PKB that differs from that with PKA. We provide a structural explanation for this difference, and highlight the ability of PKA-PKB to mimic the true PKB binding mode in this case.
The line below this paragraph, {{ABSTRACT_PUBMED_17275837}}, adds the Publication Abstract to the page
(as it appears on PubMed at http://www.pubmed.gov), where 17275837 is the PubMed ID number.
-->
{{ABSTRACT_PUBMED_17275837}}


==About this Structure==
==About this Structure==
Line 43: Line 47:
[[Category: Transferase]]
[[Category: Transferase]]
[[Category: Wnt signaling pathway]]
[[Category: Wnt signaling pathway]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 08:44:41 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 00:57:31 2008''

Revision as of 00:57, 28 July 2008

File:2jdo.png

Template:STRUCTURE 2jdo

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

Template:ABSTRACT PUBMED 17275837

About this StructureAbout this Structure

2JDO is a Protein complex structure of sequences from Homo sapiens. 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 Mon Jul 28 00:57:31 2008

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

OCA