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'''STRUCTURE OF HUMAN THR160-PHOSPHO CDK2-CYCLIN A COMPLEXED WITH A BISANILINOPYRIMIDINE INHIBITOR''' | '''STRUCTURE OF HUMAN THR160-PHOSPHO CDK2-CYCLIN A COMPLEXED WITH A BISANILINOPYRIMIDINE INHIBITOR''' | ||
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[[Category: Noble, M E.M.]] | [[Category: Noble, M E.M.]] | ||
[[Category: Pratt, D J.]] | [[Category: Pratt, D J.]] | ||
[[Category: | [[Category: Atp-binding]] | ||
[[Category: | [[Category: Cell cycle]] | ||
[[Category: | [[Category: Cell cycle complex]] | ||
[[Category: | [[Category: Cell division]] | ||
[[Category: | [[Category: Cyclin]] | ||
[[Category: | [[Category: Kinase]] | ||
[[Category: | [[Category: Mitosis]] | ||
[[Category: | [[Category: Nucleotide-binding]] | ||
[[Category: | [[Category: Phosphorylation]] | ||
[[Category: | [[Category: Polymorphism]] | ||
[[Category: | [[Category: Serine-threonine-protein kinase]] | ||
[[Category: | [[Category: Serine/threonine-protein kinase]] | ||
[[Category: | [[Category: Transferase]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 07:58:27 2008'' | |||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | |||
Revision as of 04:58, 4 May 2008
STRUCTURE OF HUMAN THR160-PHOSPHO CDK2-CYCLIN A COMPLEXED WITH A BISANILINOPYRIMIDINE INHIBITOR
Overview
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. The results indicate that certain residues that are not frequently considered in structure-aided kinase inhibitor design have an important role to play.
About this Structure
2IW9 is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.
Reference
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 Page seeded by OCA on Sun May 4 07:58:27 2008
Proteopedia Page Contributors and Editors (what is this?)
- Pages with broken file links
- Homo sapiens
- Non-specific serine/threonine protein kinase
- Protein complex
- Bentley, J.
- Boyle, F T.
- Endicott, J A.
- Jewsbury, P.
- Noble, M E.M.
- Pratt, D J.
- 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
