1urw
From Proteopedia
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|PDB= 1urw |SIZE=350|CAPTION= <scene name='initialview01'>1urw</scene>, resolution 1.6Å | |PDB= 1urw |SIZE=350|CAPTION= <scene name='initialview01'>1urw</scene>, resolution 1.6Å | ||
|SITE= <scene name='pdbsite=AC2:I1p+Binding+Site+For+Chain+A'>AC2</scene> | |SITE= <scene name='pdbsite=AC2:I1p+Binding+Site+For+Chain+A'>AC2</scene> | ||
| - | |LIGAND= <scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene> | + | |LIGAND= <scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=I1P:2-[4-(N-(3-DIMETHYLAMINOPROPYL)SULPHAMOYL)ANILINO]-'>I1P</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=1urw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1urw OCA], [http://www.ebi.ac.uk/pdbsum/1urw PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1urw RCSB]</span> | ||
}} | }} | ||
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Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors., Byth KF, Cooper N, Culshaw JD, Heaton DW, Oakes SE, Minshull CA, Norman RA, Pauptit RA, Tucker JA, Breed J, Pannifer A, Rowsell S, Stanway JJ, Valentine AL, Thomas AP, Bioorg Med Chem Lett. 2004 May 3;14(9):2249-52. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15081018 15081018] | Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors., Byth KF, Cooper N, Culshaw JD, Heaton DW, Oakes SE, Minshull CA, Norman RA, Pauptit RA, Tucker JA, Breed J, Pannifer A, Rowsell S, Stanway JJ, Valentine AL, Thomas AP, Bioorg Med Chem Lett. 2004 May 3;14(9):2249-52. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15081018 15081018] | ||
[[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: Breed, J.]] | [[Category: Breed, J.]] | ||
[[Category: Byth, K F.]] | [[Category: Byth, K F.]] | ||
| Line 38: | Line 41: | ||
[[Category: Valentine, A L.]] | [[Category: Valentine, A L.]] | ||
[[Category: Yucker, J A.]] | [[Category: Yucker, J A.]] | ||
| - | [[Category: ACE]] | ||
| - | [[Category: I1P]] | ||
[[Category: mitosis]] | [[Category: mitosis]] | ||
[[Category: serine/threonine-protein kinase]] | [[Category: serine/threonine-protein kinase]] | ||
[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:14:22 2008'' |
Revision as of 21:14, 30 March 2008
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| , resolution 1.6Å | |||||||
|---|---|---|---|---|---|---|---|
| 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 | ||||||
CDK2 IN COMPLEX WITH AN IMIDAZO[1,2-B]PYRIDAZINE
Overview
Modification of imidazo[1,2-a]pyridine CDK inhibitors lead to identification of less lipophilic imidazo[1,2-b]pyridazine series of CDK inhibitors. Although several equivalent compounds from these two series have similar structure and show similar CDK activity, the SAR of the two series differs significantly. Protein inhibitor structure determination has confirmed differences in binding mode and given some understanding of these differences in SAR. Potent and selective imidazo[1,2-b]pyridazine inhibitors of CDK2 have been identified, which show >1 microM plasma levels following a 2mg/kg oral dose to mice.
About this Structure
1URW is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors., Byth KF, Cooper N, Culshaw JD, Heaton DW, Oakes SE, Minshull CA, Norman RA, Pauptit RA, Tucker JA, Breed J, Pannifer A, Rowsell S, Stanway JJ, Valentine AL, Thomas AP, Bioorg Med Chem Lett. 2004 May 3;14(9):2249-52. PMID:15081018
Page seeded by OCA on Mon Mar 31 00:14:22 2008
Categories: Homo sapiens | Non-specific serine/threonine protein kinase | Single protein | Breed, J. | Byth, K F. | Cooper, N. | Culshaw, J D. | Heaton, D W. | Minshull, C A. | Norman, R A. | Oakes, S E. | Pannifer, A. | Pauptit, R A. | Rowsell, S. | Stanway, J J. | Thomas, A P. | Valentine, A L. | Yucker, J A. | Mitosis | Serine/threonine-protein kinase | Transferase
