4ful
From Proteopedia
(Difference between revisions)
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| - | [[ | + | ==PI3 Kinase Gamma bound to a pyrmidine inhibitor== |
| + | <StructureSection load='4ful' size='340' side='right' caption='[[4ful]], [[Resolution|resolution]] 2.47Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[4ful]] 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=4FUL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4FUL FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0VU:4-({4-[3-(PIPERIDIN-1-YLCARBONYL)PHENYL]PYRIMIDIN-2-YL}AMINO)BENZENESULFONAMIDE'>0VU</scene></td></tr> | ||
| + | <tr id='gene'><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 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=4ful FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ful OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ful RCSB], [http://www.ebi.ac.uk/pdbsum/4ful PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | hSMG-1 kinase plays a dual role in a highly conserved RNA surveillance pathway termed nonsense-mediated RNA decay (NMD) and in cellular genotoxic stress response. Since deregulation of cellular responses to stress contributes to tumor growth and resistance to chemotherapy, hSMG-1 is a potential target for cancer treatment. From our screening efforts, we have identified pyrimidine derivatives as hSMG-1 kinase inhibitors. We report structure-based optimization of this pan-kinase scaffold to improve its biochemical profile and overall kinome selectivity, including mTOR and CDK, to generate the first reported selective hSMG-1 tool compound. | ||
| - | + | Identification of pyrimidine derivatives as hSMG-1 inhibitors.,Gopalsamy A, Bennett EM, Shi M, Zhang WG, Bard J, Yu K Bioorg Med Chem Lett. 2012 Nov 1;22(21):6636-41. doi: 10.1016/j.bmcl.2012.08.107., Epub 2012 Sep 7. PMID:23021994<ref>PMID:23021994</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| + | </div> | ||
| - | + | ==See Also== | |
| - | + | *[[Phosphoinositide 3-Kinases|Phosphoinositide 3-Kinases]] | |
| - | == | + | == References == |
| - | [[ | + | <references/> |
| + | __TOC__ | ||
| + | </StructureSection> | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
| - | [[Category: Bard, J | + | [[Category: Bard, J]] |
| - | [[Category: Bennett, E M | + | [[Category: Bennett, E M]] |
| - | [[Category: Gopalsamy, A | + | [[Category: Gopalsamy, A]] |
| - | [[Category: Shi, M | + | [[Category: Shi, M]] |
| - | [[Category: Yu, K | + | [[Category: Yu, K]] |
| - | [[Category: Zhang, W G | + | [[Category: Zhang, W G]] |
[[Category: Kinase]] | [[Category: Kinase]] | ||
[[Category: Transferase-transferase inhibitor complex]] | [[Category: Transferase-transferase inhibitor complex]] | ||
Revision as of 14:51, 9 December 2014
PI3 Kinase Gamma bound to a pyrmidine inhibitor
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