4a7c
From Proteopedia
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| - | [[ | + | ==Crystal structure of PIM1 kinase with ETP46546== |
| + | <StructureSection load='4a7c' size='340' side='right' caption='[[4a7c]], [[Resolution|resolution]] 2.30Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[4a7c]] 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=4A7C OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4A7C FirstGlance]. <br> | ||
| + | </td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=E46:N-(PIPERIDIN-4-YLMETHYL)-3-[3-(TRIFLUOROMETHYLOXY)PHENYL]-[1,2,3]TRIAZOLO[4,5-B]PYRIDIN-5-AMINE'>E46</scene>, <scene name='pdbligand=IMD:IMIDAZOLE'>IMD</scene><br> | ||
| + | <tr><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene></td></tr> | ||
| + | <tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2bik|2bik]], [[2xix|2xix]], [[1ywv|1ywv]], [[2bzj|2bzj]], [[2c3i|2c3i]], [[1yxu|1yxu]], [[2j2i|2j2i]], [[1yxt|1yxt]], [[2bzh|2bzh]], [[1yxs|1yxs]], [[1xqz|1xqz]], [[1yi3|1yi3]], [[2xiz|2xiz]], [[1yxv|1yxv]], [[1xr1|1xr1]], [[2xiy|2xiy]], [[2bil|2bil]], [[1yhs|1yhs]], [[1yxx|1yxx]], [[1xws|1xws]], [[2xj1|2xj1]], [[2bzk|2bzk]], [[2xj0|2xj0]], [[2xj2|2xj2]], [[1yi4|1yi4]], [[2bzi|2bzi]]</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=4a7c FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4a7c OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4a7c RCSB], [http://www.ebi.ac.uk/pdbsum/4a7c PDBsum]</span></td></tr> | ||
| + | <table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | PIM kinases have become targets of interest due to their association with biochemical mechanisms affecting survival, proliferation and cytokine production. 1,2,3-Triazolo[4,5-b]pyridines were identified as PIM inhibitors applying a scaffold hopping approach. Initial exploration around this scaffold and X-ray crystallographic data are hereby described. | ||
| - | + | Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors.,Pastor J, Oyarzabal J, Saluste G, Alvarez RM, Rivero V, Ramos F, Cendon E, Blanco-Aparicio C, Ajenjo N, Cebria A, Albarran MI, Cebrian D, Corrionero A, Fominaya J, Montoya G, Mazzorana M Bioorg Med Chem Lett. 2012 Feb 15;22(4):1591-7. Epub 2012 Jan 5. PMID:22266039<ref>PMID:22266039</ref> | |
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| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| + | </div> | ||
| - | + | ==See Also== | |
| - | + | *[[Proto-oncogene serine/threonine-protein kinase|Proto-oncogene serine/threonine-protein kinase]] | |
| - | + | == References == | |
| - | + | <references/> | |
| - | + | __TOC__ | |
| - | + | </StructureSection> | |
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Mazzorana, M.]] | [[Category: Mazzorana, M.]] | ||
Revision as of 08:22, 5 June 2014
Crystal structure of PIM1 kinase with ETP46546
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