2a5u

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[[Image:2a5u.gif|left|200px]]
[[Image:2a5u.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2a5u |SIZE=350|CAPTION= <scene name='initialview01'>2a5u</scene>, resolution 2.700&Aring;
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The line below this paragraph, containing "STRUCTURE_2a5u", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=QYT:(5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE-2,4-DIONE'>QYT</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Phosphatidylinositol-4,5-bisphosphate_3-kinase Phosphatidylinositol-4,5-bisphosphate 3-kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.153 2.7.1.153] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_2a5u| PDB=2a5u | SCENE= }}
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|RELATEDENTRY=[[2a4z|2A4Z]], [[1e7u|1E7U]], [[1e7v|1E7V]], [[1e7w|1E7W]], [[1e8x|1E8X]], [[1e8y|1E8Y]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2a5u FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2a5u OCA], [http://www.ebi.ac.uk/pdbsum/2a5u PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2a5u RCSB]</span>
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}}
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'''Crystal Structure of human PI3Kgamma complexed with AS605240'''
'''Crystal Structure of human PI3Kgamma complexed with AS605240'''
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[[Category: Pi3kg]]
[[Category: Pi3kg]]
[[Category: Protein-inhibitor complex]]
[[Category: Protein-inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 18:38:40 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat Apr 5 19:08:25 2008''
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Revision as of 15:38, 3 May 2008

Image:2a5u.gif

Template:STRUCTURE 2a5u

Crystal Structure of human PI3Kgamma complexed with AS605240


Overview

Phosphoinositide 3-kinases (PI3K) have long been considered promising drug targets for the treatment of inflammatory and autoimmune disorders as well as cancer and cardiovascular diseases. But the lack of specificity, isoform selectivity and poor biopharmaceutical profile of PI3K inhibitors have so far hampered rigorous disease-relevant target validation. Here we describe the identification and development of specific, selective and orally active small-molecule inhibitors of PI3Kgamma (encoded by Pik3cg). We show that Pik3cg(-/-) mice are largely protected in mouse models of rheumatoid arthritis; this protection correlates with defective neutrophil migration, further validating PI3Kgamma as a therapeutic target. We also describe that oral treatment with a PI3Kgamma inhibitor suppresses the progression of joint inflammation and damage in two distinct mouse models of rheumatoid arthritis, reproducing the protective effects shown by Pik3cg(-/-) mice. Our results identify selective PI3Kgamma inhibitors as potential therapeutic molecules for the treatment of chronic inflammatory disorders such as rheumatoid arthritis.

About this Structure

2A5U is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis., Camps M, Ruckle T, Ji H, Ardissone V, Rintelen F, Shaw J, Ferrandi C, Chabert C, Gillieron C, Francon B, Martin T, Gretener D, Perrin D, Leroy D, Vitte PA, Hirsch E, Wymann MP, Cirillo R, Schwarz MK, Rommel C, Nat Med. 2005 Sep;11(9):936-43. Epub 2005 Aug 28. PMID:16127437 Page seeded by OCA on Sat May 3 18:38:40 2008

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