1urw

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[[Image:1urw.gif|left|200px]]
[[Image:1urw.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1urw |SIZE=350|CAPTION= <scene name='initialview01'>1urw</scene>, resolution 1.6&Aring;
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The line below this paragraph, containing "STRUCTURE_1urw", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC2:I1p+Binding+Site+For+Chain+A'>AC2</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=I1P:2-[4-(N-(3-DIMETHYLAMINOPROPYL)SULPHAMOYL)ANILINO]-'>I1P</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|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>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_1urw| PDB=1urw | SCENE= }}
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|RELATEDENTRY=
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|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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}}
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'''CDK2 IN COMPLEX WITH AN IMIDAZO[1,2-B]PYRIDAZINE'''
'''CDK2 IN COMPLEX WITH AN IMIDAZO[1,2-B]PYRIDAZINE'''
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[[Category: Valentine, A L.]]
[[Category: Valentine, A L.]]
[[Category: Yucker, J A.]]
[[Category: Yucker, J A.]]
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[[Category: mitosis]]
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[[Category: Mitosis]]
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[[Category: serine/threonine-protein kinase]]
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[[Category: Serine/threonine-protein kinase]]
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[[Category: transferase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 11:36:23 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:14:22 2008''
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Revision as of 08:36, 3 May 2008

Image:1urw.gif

Template:STRUCTURE 1urw

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 Sat May 3 11:36:23 2008

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OCA

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