1urw
From Proteopedia
| Line 1: | Line 1: | ||
| - | [[Image:1urw.gif|left|200px]]<br /><applet load="1urw" size=" | + | [[Image:1urw.gif|left|200px]]<br /><applet load="1urw" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1urw, resolution 1.6Å" /> | caption="1urw, resolution 1.6Å" /> | ||
'''CDK2 IN COMPLEX WITH AN IMIDAZO[1,2-B]PYRIDAZINE'''<br /> | '''CDK2 IN COMPLEX WITH AN IMIDAZO[1,2-B]PYRIDAZINE'''<br /> | ||
| Line 7: | Line 7: | ||
==About this Structure== | ==About this Structure== | ||
| - | 1URW is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with ACE and I1P as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37] Known structural/functional Site: <scene name='pdbsite=AC2:I1p Binding Site For Chain A'>AC2</scene>. Full crystallographic information is available from [http:// | + | 1URW is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=ACE:'>ACE</scene> and <scene name='pdbligand=I1P:'>I1P</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37] Known structural/functional Site: <scene name='pdbsite=AC2:I1p+Binding+Site+For+Chain+A'>AC2</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1URW OCA]. |
==Reference== | ==Reference== | ||
| Line 35: | Line 35: | ||
[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb 3 10:04:14 2008'' |
Revision as of 08:04, 3 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 Sun Feb 3 10:04:14 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
