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2oi4

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[[Image:2oi4.gif|left|200px]]
[[Image:2oi4.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2oi4 |SIZE=350|CAPTION= <scene name='initialview01'>2oi4</scene>, resolution 2.20&Aring;
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The line below this paragraph, containing "STRUCTURE_2oi4", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=EPE:4-(2-HYDROXYETHYL)-1-PIPERAZINE+ETHANESULFONIC+ACID'>EPE</scene>, <scene name='pdbligand=JM1:FLOURINATED+PYRIDOCARBAZOLE+CYCLOPENTADIENYL+RU(CO)+COMPLEX'>JM1</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[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] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= PIM1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2oi4| PDB=2oi4 | SCENE= }}
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|RELATEDENTRY=[[2bzh|2BZH]], [[2bzi|2BZI]], [[2bzj|2BZJ]], [[1yhs|1YHS]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2oi4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2oi4 OCA], [http://www.ebi.ac.uk/pdbsum/2oi4 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2oi4 RCSB]</span>
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}}
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'''Crystal structure of human PIM1 in complex with fluorinated ruthenium pyridocarbazole'''
'''Crystal structure of human PIM1 in complex with fluorinated ruthenium pyridocarbazole'''
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[[Category: Maksimoska, J.]]
[[Category: Maksimoska, J.]]
[[Category: Meggers, E.]]
[[Category: Meggers, E.]]
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[[Category: atp-binding,phosphorylation]]
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[[Category: Atp-binding,phosphorylation]]
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[[Category: transferase,pim1,kinase]]
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[[Category: Transferase,pim1,kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 10:58:22 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:18:10 2008''
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Revision as of 07:58, 4 May 2008

Image:2oi4.gif

Template:STRUCTURE 2oi4

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. 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 Sun May 4 10:58:22 2008

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