4fhj

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
-
[[Image:4fhj.png|left|200px]]
+
==Crystal Structure of PI3K-gamma in Complex with Imidazopyridine 2==
 +
<StructureSection load='4fhj' size='340' side='right' caption='[[4fhj]], [[Resolution|resolution]] 2.60&Aring;' scene=''>
 +
== Structural highlights ==
 +
<table><tr><td colspan='2'>[[4fhj]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4FHJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4FHJ FirstGlance]. <br>
 +
</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0TZ:3-(4-AMINO-6-METHYL-1,3,5-TRIAZIN-2-YL)-N-(1H-PYRAZOL-5-YL)IMIDAZO[1,2-A]PYRIDIN-2-AMINE'>0TZ</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene><br>
 +
<tr><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PIK3CG ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>
 +
<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4fhj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4fhj OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4fhj RCSB], [http://www.ebi.ac.uk/pdbsum/4fhj PDBsum]</span></td></tr>
 +
<table>
 +
<div style="background-color:#fffaf0;">
 +
== Publication Abstract from PubMed ==
 +
mTOR is a critical regulator of cellular signaling downstream of multiple growth factors. The mTOR/PI3K/AKT pathway is frequently mutated in human cancers and is thus an important oncology target. Herein we report the evolution of our program to discover ATP-competitive mTOR inhibitors that demonstrate improved pharmacokinetic properties and selectivity compared to our previous leads. Through targeted SAR and structure-guided design, new imidazopyridine and imidazopyridazine scaffolds were identified that demonstrated superior inhibition of mTOR in cellular assays, selectivity over the closely related PIKK family and improved in vivo clearance over our previously reported benzimidazole series.
-
{{STRUCTURE_4fhj| PDB=4fhj | SCENE= }}
+
Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.,Peterson EA, Boezio AA, Andrews PS, Boezio CM, Bush TL, Cheng AC, Choquette D, Coats JR, Colletti AE, Copeland KW, Dupont M, Graceffa R, Grubinska B, Kim JL, Lewis RT, Liu J, Mullady EL, Potashman MH, Romero K, Shaffer PL, Stanton MK, Stellwagen JC, Teffera Y, Yi S, Cai T, La DS Bioorg Med Chem Lett. 2012 Jun 16. PMID:22765895<ref>PMID:22765895</ref>
-
===Crystal Structure of PI3K-gamma in Complex with Imidazopyridine 2===
+
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
 +
</div>
-
{{ABSTRACT_PUBMED_22765895}}
+
==See Also==
-
 
+
*[[Phosphoinositide 3-Kinases|Phosphoinositide 3-Kinases]]
-
==About this Structure==
+
== References ==
-
[[4fhj]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4FHJ OCA].
+
<references/>
-
 
+
__TOC__
-
==Reference==
+
</StructureSection>
-
<ref group="xtra">PMID:022765895</ref><references group="xtra"/>
+
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Shaffer, P L.]]
[[Category: Shaffer, P L.]]

Revision as of 09:24, 11 June 2014

Crystal Structure of PI3K-gamma in Complex with Imidazopyridine 2

4fhj, resolution 2.60Å

Drag the structure with the mouse to rotate

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/4fhj"
Views
Personal tools
Navigation
Toolbox