2bpm
From Proteopedia
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==About this Structure== | ==About this Structure== | ||
| - | 2BPM 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 529 as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[http://en.wikipedia.org/wiki/ | + | 2BPM 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 529 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]]. Structure known Active Site: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2BPM OCA]]. |
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
| + | [[Category: Transferred entry: 2.7.11.1]] | ||
[[Category: Albanese, C.]] | [[Category: Albanese, C.]] | ||
[[Category: Alzani, R.]] | [[Category: Alzani, R.]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 10:41:11 2007'' |
Revision as of 08:36, 30 October 2007
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STRUCTURE OF CDK2-CYCLIN A WITH PHA-630529
Overview
Inhibitors of cyclin-dependent kinases (CDK) such as CDK2/cyclin A-E are, currently undergoing clinical trials to verify their potential as new, anticancer agents. In a previous article we described the lead discovery, process of a 3-aminopyrazole class of CDK2/cyclin A-E inhibitors. The, endpoint of this process was PNU-292137, a compound endowed with in vivo, antitumor activity in a mouse tumor xenograft model. We optimized this, lead compound to improve some physicochemical properties, notably, solubility and plasma protein binding. This lead optimization process, brought us to the discovery of, (2S)-N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-[4-(2-oxo-1-pyrrolidinyl)phenyl]p, ropanamide (PHA-533533, 13), a compound with a balanced activity vs, druglike profile. Compound 13 inhibited ... [(full description)]
About this Structure
2BPM is a [Protein complex] structure of sequences from [Homo sapiens] with SO4 and 529 as [ligands]. Active as [Transferred entry: 2.7.11.1], with EC number [2.7.1.37]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].
Reference
3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization., Pevarello P, Brasca MG, Orsini P, Traquandi G, Longo A, Nesi M, Orzi F, Piutti C, Sansonna P, Varasi M, Cameron A, Vulpetti A, Roletto F, Alzani R, Ciomei M, Albanese C, Pastori W, Marsiglio A, Pesenti E, Fiorentini F, Bischoff JR, Mercurio C, J Med Chem. 2005 Apr 21;48(8):2944-56. PMID:15828833
Page seeded by OCA on Tue Oct 30 10:41:11 2007
Categories: Homo sapiens | Protein complex | Transferred entry: 2.7.11.1 | Albanese, C. | Alzani, R. | Bischoff, J.R. | Brasca, M.G. | Cameron, A. | Ciomei, M. | Fiorentini, F. | Fogliatto, G. | Longo, A. | Marsiglio, A. | Mercurio, C. | Nesi, M. | Orsini, P. | Orzi, F. | Pastori, W. | Pesenti, E. | Pevarello, P. | Piutti, C. | Roletto, F. | Sansonna, P. | Traquandi, G. | Varasi, M. | Vulpetti, A. | 529 | SO4 | Cell division | Cyclin | Phosphorylation | Protein kinase | Serine/threonine-protein kinase | Transferase
