1oiq
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| , resolution 2.31Å | |||||||
|---|---|---|---|---|---|---|---|
| Sites: | |||||||
| Ligands: | |||||||
| Activity: | Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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. 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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- Homo sapiens
- Non-specific serine/threonine protein kinase
- Single protein
- 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.
- Atp-binding
- Cell cycle
- Cell division
- Mitosis
- Phosphorylation,
- Protein kinase
- Serine/threonine-protein kinase
- Transferase