2j4z
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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.
About this StructureAbout 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.
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
Page seeded by OCA on Mon Nov 5 18:25:14 2007
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- 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