2j4z
From Proteopedia
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==About this Structure== | ==About this Structure== | ||
| - | 2J4Z is a | + | 2J4Z 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 626 and ARS as [http://en.wikipedia.org/wiki/ligands ligands]. Structure known Active Site: AC1. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2J4Z OCA]. |
==Reference== | ==Reference== | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 14:57:39 2007'' |
Revision as of 12:52, 5 November 2007
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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 with 626 and ARS as ligands. Structure known Active Site: AC1. 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 Mon Nov 5 14:57:39 2007
Categories: Homo sapiens | Single protein | Berta, D. | Bindi, S. | Cameron, A.D. | Fancelli, D. | Forte, B. | Izzo, G. | Rusconi, L. | Severino, D. | Storici, P. | Tonani, R. | Varasi, M. | Vianello, P. | 626 | ARS | Atp-binding | Cell cycle | Kinase | Nucleotide- binding | Nucleotide-binding | Phosphorylation | Serine-threonine-protein kinase | Serine/threonine-protein kinase | Transferase
