2j4z

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[[Image:2j4z.jpg|left|200px]]
[[Image:2j4z.jpg|left|200px]]
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{{Structure
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|PDB= 2j4z |SIZE=350|CAPTION= <scene name='initialview01'>2j4z</scene>, resolution 2.00&Aring;
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The line below this paragraph, containing "STRUCTURE_2j4z", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Ars+Binding+Site+For+Chain+A'>AC1</scene>
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|LIGAND= <scene name='pdbligand=626:4-(4-METHYLPIPERAZIN-1-YL)-N-[5-(2-THIENYLACETYL)-1,5-DIHYDROPYRROLO[3,4-C]PYRAZOL-3-YL]BENZAMIDE'>626</scene>, <scene name='pdbligand=ARS:ARSENIC'>ARS</scene>
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{{STRUCTURE_2j4z| PDB=2j4z | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2j4z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2j4z OCA], [http://www.ebi.ac.uk/pdbsum/2j4z PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2j4z RCSB]</span>
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}}
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'''STRUCTURE OF AURORA-2 IN COMPLEX WITH PHA-680626'''
'''STRUCTURE OF AURORA-2 IN COMPLEX WITH PHA-680626'''
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[[Category: Varasi, M.]]
[[Category: Varasi, M.]]
[[Category: Vianello, P.]]
[[Category: Vianello, P.]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: cell cycle]]
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[[Category: Cell cycle]]
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[[Category: kinase]]
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[[Category: Kinase]]
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[[Category: nucleotide- binding]]
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[[Category: Nucleotide- binding]]
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[[Category: nucleotide-binding]]
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[[Category: Nucleotide-binding]]
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[[Category: phosphorylation]]
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[[Category: Phosphorylation]]
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[[Category: serine-threonine-protein kinase]]
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[[Category: Serine-threonine-protein kinase]]
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[[Category: serine/threonine-protein kinase]]
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[[Category: Serine/threonine-protein kinase]]
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[[Category: transferase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 08:20:26 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:53:01 2008''
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Revision as of 05:20, 4 May 2008

Image:2j4z.jpg

Template:STRUCTURE 2j4z

STRUCTURE OF AURORA-2 IN COMPLEX WITH PHA-680626


Overview

The optimization of a series of 5-phenylacetyl 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole derivatives toward the inhibition of Aurora kinases led to the identification of compound 9d. This is a potent inhibitor of Aurora kinases that also shows low nanomolar potency against additional anticancer kinase targets. Based on its high antiproliferative activity on different cancer cell lines, favorable chemico-physical and pharmacokinetic properties, and high efficacy in in vivo tumor models, compound 9d was ultimately selected for further development.

About this Structure

2J4Z is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile., Fancelli D, Moll J, Varasi M, Bravo R, Artico R, Berta D, Bindi S, Cameron A, Candiani I, Cappella P, Carpinelli P, Croci W, Forte B, Giorgini ML, Klapwijk J, Marsiglio A, Pesenti E, Rocchetti M, Roletto F, Severino D, Soncini C, Storici P, Tonani R, Zugnoni P, Vianello P, J Med Chem. 2006 Nov 30;49(24):7247-51. PMID:17125279 Page seeded by OCA on Sun May 4 08:20:26 2008

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OCA

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