2bkz
From Proteopedia
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==Overview== | ==Overview== | ||
| - | The synthesis and the preliminary expansion of this new class of CDK2 | + | 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== | ==About this Structure== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
| - | [[Category: Transferred entry: 2 | + | [[Category: Transferred entry: 2 7.11 1]] |
[[Category: Bargiottia, A.]] | [[Category: Bargiottia, A.]] | ||
| - | [[Category: Brasca, M | + | [[Category: Brasca, M G.]] |
[[Category: Cameron, A.]] | [[Category: Cameron, A.]] | ||
[[Category: Dalessio, R.]] | [[Category: Dalessio, R.]] | ||
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[[Category: Roletto, F.]] | [[Category: Roletto, F.]] | ||
[[Category: Tibolla, M.]] | [[Category: Tibolla, M.]] | ||
| - | [[Category: Vazquez, M | + | [[Category: Vazquez, M L.]] |
[[Category: Vulpetti, A.]] | [[Category: Vulpetti, A.]] | ||
[[Category: SBC]] | [[Category: SBC]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:38:53 2008'' |
Revision as of 14:38, 21 February 2008
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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 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
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 Feb 21 16:38:53 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
