2iw6
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STRUCTURE OF HUMAN THR160-PHOSPHO CDK2-CYCLIN A COMPLEXED WITH A BISANILINOPYRIMIDINE INHIBITOR
OverviewOverview
Cyclin dependent kinases are a key family of kinases involved in cell, cycle regulation and are an attractive target for cancer chemotherapy. The, roles of four residues of the cyclin-dependent kinase active site in, inhibitor selectivity were investigated by producing cyclin-dependent, kinase 2 mutants bearing equivalent cyclin-dependent kinase 4 residues, namely F82H, L83V, H84D, and K89T. Assay of the mutants with a, cyclin-dependent kinase 4-selective bisanilinopyrimidine shows that the, K89T mutation is primarily responsible for the selectivity of this, compound. Use of the cyclin-dependent kinase 2-selective, 6-cyclohexylmethoxy-2-(4'-sulfamoylanilino)purine (NU6102) shows that K89T, has no role in the selectivity, while the remaining three mutations have a, cumulative influence. ... [(full description)]
About this StructureAbout this Structure
2IW6 is a [Protein complex] structure of sequences from [Homo sapiens] with MG, QQ2 and SGM as [ligands]. Active as [[1]], with EC number [2.7.1.37]. Full crystallographic information is available from [OCA].
ReferenceReference
Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity., Pratt DJ, Bentley J, Jewsbury P, Boyle FT, Endicott JA, Noble ME, J Med Chem. 2006 Sep 7;49(18):5470-7. PMID:16942020
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- Homo sapiens
- Protein complex
- Bentley, J.
- Boyle, F.T.
- Endicott, J.A.
- Jewsbury, P.
- Noble, M.E.M.
- Pratt, D.J.
- MG
- QQ2
- SGM
- Atp-binding
- Cell cycle
- Cell cycle complex
- Cell division
- Cyclin
- Kinase
- Mitosis
- Nucleotide-binding
- Phosphorylation
- Polymorphism
- Serine-threonine-protein kinase
- Serine/threonine-protein kinase
- Transferase