2j50

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{{STRUCTURE_2j50| PDB=2j50 | SCENE= }}
{{STRUCTURE_2j50| PDB=2j50 | SCENE= }}
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'''STRUCTURE OF AURORA-2 IN COMPLEX WITH PHA-739358'''
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===STRUCTURE OF AURORA-2 IN COMPLEX WITH PHA-739358===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 17125279 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17125279}}
==About this Structure==
==About this Structure==
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[[Category: Serine/threonine-protein kinase]]
[[Category: Serine/threonine-protein kinase]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 08:20:36 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 18:27:35 2008''

Revision as of 15:27, 28 July 2008

Image:2j50.png

Template:STRUCTURE 2j50

STRUCTURE OF AURORA-2 IN COMPLEX WITH PHA-739358

Template:ABSTRACT PUBMED 17125279

About this Structure

2J50 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

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