2bkz
From Proteopedia
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| , resolution 2.60Å | |||||||
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| Sites: | |||||||
| Ligands: | , | ||||||
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| 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 Mon Mar 31 02:07:55 2008
Categories: Homo sapiens | Non-specific serine/threonine protein kinase | Protein complex | 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. | Atp-binding | Cell cycle | Cell division | Cyclin | Mitosis | Phosphorylation | Polymorphism | Protein kinase | Serine/threonine-protein kinase | Transferase
