2jdo

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
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 21:57, 27 July 2008

Image:2jdo.png

Template:STRUCTURE 2jdo

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

Template:ABSTRACT PUBMED 17275837

About this Structure

2JDO is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from 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:17275837

Page seeded by OCA on Mon Jul 28 00:57:31 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2jdo"
Personal tools