2j4z: Difference between revisions
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[[Image:2j4z.jpg|left|200px]]<br /><applet load="2j4z" size=" | [[Image:2j4z.jpg|left|200px]]<br /><applet load="2j4z" size="350" color="white" frame="true" align="right" spinBox="true" | ||
caption="2j4z, resolution 2.00Å" /> | caption="2j4z, resolution 2.00Å" /> | ||
'''STRUCTURE OF AURORA-2 IN COMPLEX WITH PHA-680626'''<br /> | '''STRUCTURE OF AURORA-2 IN COMPLEX WITH PHA-680626'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
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]. Known structural/functional Site: <scene name='pdbsite=AC1:Ars Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http:// | 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 <scene name='pdbligand=626:'>626</scene> and <scene name='pdbligand=ARS:'>ARS</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Known structural/functional Site: <scene name='pdbsite=AC1:Ars+Binding+Site+For+Chain+A'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2J4Z OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb 3 10:41:38 2008'' | ||
Revision as of 11:41, 3 February 2008
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STRUCTURE OF AURORA-2 IN COMPLEX WITH PHA-680626
OverviewOverview
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.
DiseaseDisease
Known diseases associated with this structure: Colon cancer, susceptibility to OMIM:[603072]
About this StructureAbout this Structure
2J4Z is a Single protein structure of sequence from Homo sapiens with and as ligands. Known structural/functional Site: . Full crystallographic information is available from OCA.
ReferenceReference
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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Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCA- Pages with broken file links
- 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