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2oi4
From Proteopedia
(New page: 200px<br /> <applet load="2oi4" size="450" color="white" frame="true" align="right" spinBox="true" caption="2oi4, resolution 2.20Å" /> '''Crystal structure o...) |
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| - | [[Image:2oi4.gif|left|200px]]<br /> | + | [[Image:2oi4.gif|left|200px]]<br /><applet load="2oi4" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2oi4" size=" | + | |
caption="2oi4, resolution 2.20Å" /> | caption="2oi4, resolution 2.20Å" /> | ||
'''Crystal structure of human PIM1 in complex with fluorinated ruthenium pyridocarbazole'''<br /> | '''Crystal structure of human PIM1 in complex with fluorinated ruthenium pyridocarbazole'''<br /> | ||
| + | |||
| + | ==Overview== | ||
| + | A general route to ruthenium pyridocarbazole half-sandwich complexes is, presented and applied to the synthesis of sixteen new compounds, many of, which have modulated protein kinase inhibition properties. For example, the incorporation of a fluorine into the pyridine moiety increases the, binding affinity for glycogen synthase kinase 3 by almost one order of, magnitude. These data are supplemented with cyclic voltammetry experiments, and a protein co-crystallographic study. | ||
==About this Structure== | ==About this Structure== | ||
| - | 2OI4 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with CL, JM1, EDO and EPE as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] Full crystallographic information is available from [http:// | + | 2OI4 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=CL:'>CL</scene>, <scene name='pdbligand=JM1:'>JM1</scene>, <scene name='pdbligand=EDO:'>EDO</scene> and <scene name='pdbligand=EPE:'>EPE</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2OI4 OCA]. |
| + | |||
| + | ==Reference== | ||
| + | Ruthenium half-sandwich complexes as protein kinase inhibitors: derivatization of the pyridocarbazole pharmacophore ligand., Pagano N, Maksimoska J, Bregman H, Williams DS, Webster RD, Xue F, Meggers E, Org Biomol Chem. 2007 Apr 21;5(8):1218-27. Epub 2007 Mar 20. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17406720 17406720] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Non-specific serine/threonine protein kinase]] | [[Category: Non-specific serine/threonine protein kinase]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:03:21 2008'' |
Revision as of 10:03, 23 January 2008
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Crystal structure of human PIM1 in complex with fluorinated ruthenium pyridocarbazole
Overview
A general route to ruthenium pyridocarbazole half-sandwich complexes is, presented and applied to the synthesis of sixteen new compounds, many of, which have modulated protein kinase inhibition properties. For example, the incorporation of a fluorine into the pyridine moiety increases the, binding affinity for glycogen synthase kinase 3 by almost one order of, magnitude. These data are supplemented with cyclic voltammetry experiments, and a protein co-crystallographic study.
About this Structure
2OI4 is a Single protein structure of sequence from Homo sapiens with , , and as ligands. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Full crystallographic information is available from OCA.
Reference
Ruthenium half-sandwich complexes as protein kinase inhibitors: derivatization of the pyridocarbazole pharmacophore ligand., Pagano N, Maksimoska J, Bregman H, Williams DS, Webster RD, Xue F, Meggers E, Org Biomol Chem. 2007 Apr 21;5(8):1218-27. Epub 2007 Mar 20. PMID:17406720
Page seeded by OCA on Wed Jan 23 12:03:21 2008
Categories: Homo sapiens | Non-specific serine/threonine protein kinase | Single protein | Maksimoska, J. | Meggers, E. | CL | EDO | EPE | JM1 | Atp-binding | Kinase | Phosphorylation | Pim1 | Transferase
