1oit
From Proteopedia
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|SITE= <scene name='pdbsite=AC1:Hdt+Binding+Site+For+Chain+A'>AC1</scene> | |SITE= <scene name='pdbsite=AC1:Hdt+Binding+Site+For+Chain+A'>AC1</scene> | ||
|LIGAND= <scene name='pdbligand=HDT:4-[(4-IMIDAZO[1,2-A]PYRIDIN-3-YLPYRIMIDIN-2-YL)AMINO]BENZENESULFONAMIDE'>HDT</scene> | |LIGAND= <scene name='pdbligand=HDT:4-[(4-IMIDAZO[1,2-A]PYRIDIN-3-YLPYRIMIDIN-2-YL)AMINO]BENZENESULFONAMIDE'>HDT</scene> | ||
| - | |ACTIVITY= [http://en.wikipedia.org/wiki/ | + | |ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span> |
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY= | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1oit FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1oit OCA], [http://www.ebi.ac.uk/pdbsum/1oit PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1oit RCSB]</span> | ||
}} | }} | ||
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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:[http://www.ncbi.nlm.nih.gov/pubmed/12941325 12941325] | 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:[http://www.ncbi.nlm.nih.gov/pubmed/12941325 12941325] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
| + | [[Category: Non-specific serine/threonine protein kinase]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Transferred entry: 2 7.11 1]] | ||
[[Category: Beattie, J F.]] | [[Category: Beattie, J F.]] | ||
[[Category: Breault, G A.]] | [[Category: Breault, G A.]] | ||
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[[Category: Pauptit, R A.]] | [[Category: Pauptit, R A.]] | ||
[[Category: Thomas, A P.]] | [[Category: Thomas, A P.]] | ||
| - | [[Category: HDT]] | ||
[[Category: protein kinase]] | [[Category: protein kinase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:45:58 2008'' |
Revision as of 19:45, 30 March 2008
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| , resolution 1.60Å | |||||||
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| 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
Overview
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 Structure
1OIT is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
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
Page seeded by OCA on Sun Mar 30 22:45:58 2008
