1oiq
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IMIDAZOPYRIDINES: A POTENT AND SELECTIVE CLASS OF CYCLIN-DEPENDENT KINASE INHIBITORS IDENTIFIED THROUGH STRUCTURE-BASED HYBRIDISATION
OverviewOverview
High-throughput screening identified the imidazo[1,2-a]pyridine and, bisanilinopyrimidine series as inhibitors of the cyclin-dependent kinase, CDK4. Comparison of their experimentally-determined binding modes and, emerging structure-activity trends led to the development of potent and, selective imidazo[1,2-a]pyridine inhibitors for CDK4 and in particular, CDK2.
About this StructureAbout this Structure
1OIQ is a [Single protein] structure of sequence from [Homo sapiens] with HDU as [ligand]. 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].
ReferenceReference
Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation., Anderson M, Beattie JF, Breault GA, Breed J, Byth KF, Culshaw JD, Ellston RP, Green S, Minshull CA, Norman RA, Pauptit RA, Stanway J, Thomas AP, Jewsbury PJ, Bioorg Med Chem Lett. 2003 Sep 15;13(18):3021-6. PMID:12941325
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OCA- Pages with broken file links
- Homo sapiens
- Single protein
- Transferred entry: 2.7.11.1
- Beattie, J.F.
- Breault, G.A.
- Byth, K.F.
- Culshaw, J.D.
- Ellston, R.P.A.
- Green, S.
- Jewsbury, P.J.
- Minshull, C.A.
- Norman, R.A.
- Pauptit, R.A.
- Thomas, A.P.
- HDU
- Atp-binding
- Cell cycle
- Cell division
- Mitosis
- Phosphorylation
- Protein kinase
- Serine/threonine-protein kinase
- Transferase