2c4g
From Proteopedia
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| - | [[Image:2c4g.gif|left|200px]]<br /><applet load="2c4g" size=" | + | [[Image:2c4g.gif|left|200px]]<br /><applet load="2c4g" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="2c4g, resolution 2.70Å" /> | caption="2c4g, resolution 2.70Å" /> | ||
'''STRUCTURE OF CDK2-CYCLIN A WITH PHA-533514'''<br /> | '''STRUCTURE OF CDK2-CYCLIN A WITH PHA-533514'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2C4G is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SO4 and 514 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37] Known structural/functional Site: <scene name='pdbsite=AC1:So4 Binding Site For Chain D'>AC1</scene>. Full crystallographic information is available from [http:// | + | 2C4G is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=SO4:'>SO4</scene> and <scene name='pdbligand=514:'>514</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37] Known structural/functional Site: <scene name='pdbsite=AC1:So4+Binding+Site+For+Chain+D'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2C4G 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 10:31:21 2008'' |
Revision as of 08:31, 3 February 2008
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STRUCTURE OF CDK2-CYCLIN A WITH PHA-533514
Overview
We have recently reported about a new class of Aurora-A inhibitors based, on a bicyclic tetrahydropyrrolo[3,4-c]pyrazole scaffold. Here we describe, the synthesis and early expansion of CDK2/cyclin A-E inhibitors belonging, to the same chemical class. Synthesis of the compounds was accomplished, using a solution-phase protocol amenable to rapid parallel expansion., Compounds with nanomolar activity in the biochemical assay and able to, efficiently inhibit CDK2-mediated tumor cell proliferation have been, obtained.
About this Structure
2C4G is a Protein complex structure of sequences from Homo sapiens with and as ligands. Active as Transferred entry: 2.7.11.1, with EC number 2.7.1.37 Known structural/functional Site: . Full crystallographic information is available from OCA.
Reference
3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors., Pevarello P, Fancelli D, Vulpetti A, Amici R, Villa M, Pittala V, Vianello P, Cameron A, Ciomei M, Mercurio C, Bischoff JR, Roletto F, Varasi M, Brasca MG, Bioorg Med Chem Lett. 2006 Feb 15;16(4):1084-90. Epub 2005 Nov 14. PMID:16290148
Page seeded by OCA on Sun Feb 3 10:31:21 2008
Categories: Homo sapiens | Protein complex | Transferred entry: 2.7.11.1 | Amici, R. | Bischoff, J.R. | Brasca, M.G. | Cameron, A. | Ciomei, M. | Fancelli, D. | Fogliatto, G. | Mercurio, C. | Pevarello, P. | Pittala, V. | Roletto, F. | Varasi, M. | Villa, M. | Vulpetti, A. | 514 | SO4 | Atp-binding | Cell cycle | Cell division | Cyclin | Mitosis | Nucleotide-binding | Phosphorylation | Polymorphism | Protein kinase | Serine/threonine-protein kinase | Transferase
