1q3d

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
[[Image:1q3d.gif|left|200px]]
[[Image:1q3d.gif|left|200px]]
-
{{Structure
+
<!--
-
|PDB= 1q3d |SIZE=350|CAPTION= <scene name='initialview01'>1q3d</scene>, resolution 2.20&Aring;
+
The line below this paragraph, containing "STRUCTURE_1q3d", creates the "Structure Box" on the page.
-
|SITE=
+
You may change the PDB parameter (which sets the PDB file loaded into the applet)
-
|LIGAND= <scene name='pdbligand=STU:STAUROSPORINE'>STU</scene>
+
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-
|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>
+
or leave the SCENE parameter empty for the default display.
-
|GENE= GSK3B ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
+
-->
-
|DOMAIN=
+
{{STRUCTURE_1q3d| PDB=1q3d | SCENE= }}
-
|RELATEDENTRY=[[1pyx|1PYX]]
+
-
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1q3d FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1q3d OCA], [http://www.ebi.ac.uk/pdbsum/1q3d PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1q3d RCSB]</span>
+
-
}}
+
'''GSK-3 Beta complexed with Staurosporine'''
'''GSK-3 Beta complexed with Staurosporine'''
Line 34: Line 31:
[[Category: Valsasina, B.]]
[[Category: Valsasina, B.]]
[[Category: Vulpetti, A.]]
[[Category: Vulpetti, A.]]
-
[[Category: insulin pathway]]
+
[[Category: Insulin pathway]]
-
[[Category: kinase]]
+
[[Category: Kinase]]
-
 
+
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 05:49:03 2008''
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:08:17 2008''
+

Revision as of 02:49, 3 May 2008

Image:1q3d.gif

Template:STRUCTURE 1q3d

GSK-3 Beta complexed with Staurosporine


Overview

GSK-3beta is a regulatory serine/threonine kinase with a plethora of cellular targets. Consequently, selective small molecule inhibitors of GSK-3beta may have a variety of therapeutic uses including the treatment of neurodegenerative diseases, type II diabetes and cancer. In order to characterize the active site of GSK-3beta, we determined crystal structures of unphosphorylated GSK-3beta in complex with selective and non-selective ATP-mimetic inhibitors. Analysis of the inhibitors' interactions with GSK-3beta in the structures reveals how the enzyme can accommodate a number of diverse molecular scaffolds. In addition, a conserved water molecule near Thr138 is identified that can serve a functional role in inhibitor binding. Finally, a comparison of the interactions made by selective and non-selective inhibitors highlights residues on the edge of the ATP binding-site that can be used to obtain inhibitor selectivity. Information gained from these structures provides a promising route for the design of second-generation GSK-3beta inhibitors.

About this Structure

1Q3D is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structural characterization of the GSK-3beta active site using selective and non-selective ATP-mimetic inhibitors., Bertrand JA, Thieffine S, Vulpetti A, Cristiani C, Valsasina B, Knapp S, Kalisz HM, Flocco M, J Mol Biol. 2003 Oct 17;333(2):393-407. PMID:14529625 Page seeded by OCA on Sat May 3 05:49:03 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1q3d"
Personal tools