2bkz
From Proteopedia
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| - | [[Image:2bkz.gif|left|200px]] | + | [[Image:2bkz.gif|left|200px]] |
| - | + | ||
| - | '''STRUCTURE OF CDK2-CYCLIN A WITH PHA-404611''' | + | {{Structure |
| + | |PDB= 2bkz |SIZE=350|CAPTION= <scene name='initialview01'>2bkz</scene>, resolution 2.60Å | ||
| + | |SITE= <scene name='pdbsite=AC1:So4+Binding+Site+For+Chain+D'>AC1</scene> | ||
| + | |LIGAND= <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene> and <scene name='pdbligand=SBC:1-[4-(AMINOSULFONYL)PHENYL]-1,6-DIHYDROPYRAZOLO[3,4-E]INDAZOLE-3-CARBOXAMIDE'>SBC</scene> | ||
| + | |ACTIVITY= [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] | ||
| + | |GENE= | ||
| + | }} | ||
| + | |||
| + | '''STRUCTURE OF CDK2-CYCLIN A WITH PHA-404611''' | ||
| + | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2BKZ is a [ | + | 2BKZ is a [[Protein complex]] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2BKZ OCA]. |
==Reference== | ==Reference== | ||
| - | Benzodipyrazoles: a new class of potent CDK2 inhibitors., D'Alessio R, Bargiotti A, Metz S, Brasca MG, Cameron A, Ermoli A, Marsiglio A, Polucci P, Roletto F, Tibolla M, Vazquez ML, Vulpetti A, Pevarello P, Bioorg Med Chem Lett. 2005 Mar 1;15(5):1315-9. PMID:[http:// | + | Benzodipyrazoles: a new class of potent CDK2 inhibitors., D'Alessio R, Bargiotti A, Metz S, Brasca MG, Cameron A, Ermoli A, Marsiglio A, Polucci P, Roletto F, Tibolla M, Vazquez ML, Vulpetti A, Pevarello P, Bioorg Med Chem Lett. 2005 Mar 1;15(5):1315-9. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15713378 15713378] |
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 16:03:20 2008'' |
Revision as of 14:03, 20 March 2008
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| , resolution 2.60Å | |||||||
|---|---|---|---|---|---|---|---|
| Sites: | |||||||
| Ligands: | and | ||||||
| Activity: | Transferred entry: 2.7.11.1, with EC number 2.7.1.37 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
STRUCTURE OF CDK2-CYCLIN A WITH PHA-404611
Overview
The synthesis and the preliminary expansion of this new class of CDK2 inhibitors are presented. The synthesis was accomplished using a solution-phase protocol amenable to rapid parallel expansion and suitable to be scaled-up in view of possible lead development. Following a medicinal chemistry program aimed at improving cell permeability and selectivity, a series of compounds with nanomolar activity in the biochemical assay and able to efficiently inhibit tumor cell proliferation has been obtained.
About this Structure
2BKZ is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Benzodipyrazoles: a new class of potent CDK2 inhibitors., D'Alessio R, Bargiotti A, Metz S, Brasca MG, Cameron A, Ermoli A, Marsiglio A, Polucci P, Roletto F, Tibolla M, Vazquez ML, Vulpetti A, Pevarello P, Bioorg Med Chem Lett. 2005 Mar 1;15(5):1315-9. PMID:15713378
Page seeded by OCA on Thu Mar 20 16:03:20 2008
Categories: Homo sapiens | Protein complex | Transferred entry: 2 7.11 1 | Bargiottia, A. | Brasca, M G. | Cameron, A. | Dalessio, R. | Ermoli, A. | Marsiglio, A. | Metz, S. | Pevarello, P. | Polucci, P. | Roletto, F. | Tibolla, M. | Vazquez, M L. | Vulpetti, A. | SBC | SO4 | Atp-binding | Cell cycle | Cell division | Cyclin | Mitosis | Phosphorylation | Polymorphism | Protein kinase | Serine/threonine-protein kinase | Transferase
