2c4g | pdb_00002c4g
STRUCTURE OF CDK2-CYCLIN A WITH PHA-533514
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Overview
We have recently reported about a new class of Aurora-A inhibitors based, on a bicyclic tetrahydropyrrolo[3,4-c]pyrazole scaffold. Here we describe, the synthesis and early expansion of CDK2/cyclin A-E inhibitors belonging, to the same chemical class. Synthesis of the compounds was accomplished, using a solution-phase protocol amenable to rapid parallel expansion., Compounds with nanomolar activity in the biochemical assay and able to, efficiently inhibit CDK2-mediated tumor cell proliferation have been, obtained.
About this Structure
2C4G is a [Protein complex] structure of sequences from [Homo sapiens] with SO4 and 514 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-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors., Pevarello P, Fancelli D, Vulpetti A, Amici R, Villa M, Pittala V, Vianello P, Cameron A, Ciomei M, Mercurio C, Bischoff JR, Roletto F, Varasi M, Brasca MG, Bioorg Med Chem Lett. 2006 Feb 15;16(4):1084-90. Epub 2005 Nov 14. PMID:16290148
Page seeded by OCA on Tue Oct 30 12:14:21 2007
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- Homo sapiens
- Protein complex
- Transferred entry: 2.7.11.1
- Amici, R.
- Bischoff, J.R.
- Brasca, M.G.
- Cameron, A.
- Ciomei, M.
- Fancelli, D.
- Fogliatto, G.
- Mercurio, C.
- Pevarello, P.
- Pittala, V.
- Roletto, F.
- Varasi, M.
- Villa, M.
- Vulpetti, A.
- 514
- SO4
- Atp-binding
- Cell cycle
- Cell division
- Cyclin
- Mitosis
- Nucleotide-binding
- Phosphorylation
- Polymorphism
- Protein kinase
- Serine/threonine-protein kinase
- Transferase
