4urk
From Proteopedia
(Difference between revisions)
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| - | ''' | + | ==PI3Kg in complex with AZD6482== |
| + | <StructureSection load='4urk' size='340' side='right' caption='[[4urk]], [[Resolution|resolution]] 2.90Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[4urk]] 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=4URK OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4URK FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=A82:2-[[(1R)-1-(7-METHYL-2-MORPHOLIN-4-YL-4-OXIDANYLIDENE-PYRIDO[1,2-A]PYRIMIDIN-9-YL)ETHYL]AMINO]BENZOIC+ACID'>A82</scene></td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4urk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4urk OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4urk RCSB], [http://www.ebi.ac.uk/pdbsum/4urk PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Optimization of AZD6482 (2), the first antiplatelet PI3Kbeta inhibitor evaluated in man, focused on improving the pharmacokinetic profile to a level compatible with once daily oral dosing as well as achieving adequate selectivity towards PI3Kalpha to minimize the risk for insulin resistance. Structure-based design and optimization of DMPK properties resulted in (R)-16, a novel, orally bioavailable PI3Kbeta inhibitor with potent in vivo anti-thrombotic effect with excellent separation to bleeding risk and insulin resistance. | ||
| - | + | Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3Kbeta inhibitors, useful as antiplatelet agents.,Giordanetto F, Barlaam B, Berglund S, Edman K, Karlsson O, Lindberg J, Nylander S, Inghardt T Bioorg Med Chem Lett. 2014 Aug 15;24(16):3936-43. doi:, 10.1016/j.bmcl.2014.07.007. Epub 2014 Jul 9. PMID:25042253<ref>PMID:25042253</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | + | == References == | |
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Barlaam, B.]] | ||
| + | [[Category: Berglund, S.]] | ||
| + | [[Category: Edman, K.]] | ||
| + | [[Category: Giordanetto, F.]] | ||
| + | [[Category: Inghardt, T.]] | ||
| + | [[Category: Karlsson, O.]] | ||
| + | [[Category: Lindberg, J.]] | ||
| + | [[Category: Nylander, S.]] | ||
| + | [[Category: Lipid kinase]] | ||
| + | [[Category: Transferase]] | ||
Revision as of 12:30, 22 October 2014
PI3Kg in complex with AZD6482
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