1urw
From Proteopedia
| Line 4: | Line 4: | ||
==Overview== | ==Overview== | ||
| - | Modification of imidazo[1,2-a]pyridine CDK inhibitors lead to | + | 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== | ==About this Structure== | ||
| Line 13: | Line 13: | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Transferred entry: 2 | + | [[Category: Transferred entry: 2 7.11 1]] |
[[Category: Breed, J.]] | [[Category: Breed, J.]] | ||
| - | [[Category: Byth, K | + | [[Category: Byth, K F.]] |
[[Category: Cooper, N.]] | [[Category: Cooper, N.]] | ||
| - | [[Category: Culshaw, J | + | [[Category: Culshaw, J D.]] |
| - | [[Category: Heaton, D | + | [[Category: Heaton, D W.]] |
| - | [[Category: Minshull, C | + | [[Category: Minshull, C A.]] |
| - | [[Category: Norman, R | + | [[Category: Norman, R A.]] |
| - | [[Category: Oakes, S | + | [[Category: Oakes, S E.]] |
[[Category: Pannifer, A.]] | [[Category: Pannifer, A.]] | ||
| - | [[Category: Pauptit, R | + | [[Category: Pauptit, R A.]] |
[[Category: Rowsell, S.]] | [[Category: Rowsell, S.]] | ||
| - | [[Category: Stanway, J | + | [[Category: Stanway, J J.]] |
| - | [[Category: Thomas, A | + | [[Category: Thomas, A P.]] |
| - | [[Category: Valentine, A | + | [[Category: Valentine, A L.]] |
| - | [[Category: Yucker, J | + | [[Category: Yucker, J A.]] |
[[Category: ACE]] | [[Category: ACE]] | ||
[[Category: I1P]] | [[Category: I1P]] | ||
| Line 35: | Line 35: | ||
[[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 Thu Feb 21 15:27:38 2008'' |
Revision as of 13:27, 21 February 2008
|
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 with and as ligands. Active as Transferred entry: 2.7.11.1, with EC number 2.7.1.37 Known structural/functional Site: . 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 Thu Feb 21 15:27:38 2008
Categories: Homo sapiens | Single protein | Transferred entry: 2 7.11 1 | 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. | ACE | I1P | Mitosis | Serine/threonine-protein kinase | Transferase
