This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.
Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.
2bkz
From Proteopedia
|
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 SO4 and SBC 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
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 Tue Oct 30 14:07:21 2007
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
