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 Known structural/functional 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 Thu Feb 21 16:44:45 2008
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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
