1urw

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[[Image:1urw.gif|left|200px]]
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{{STRUCTURE_1urw| PDB=1urw | SCENE= }}
{{STRUCTURE_1urw| PDB=1urw | SCENE= }}
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'''CDK2 IN COMPLEX WITH AN IMIDAZO[1,2-B]PYRIDAZINE'''
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===CDK2 IN COMPLEX WITH AN IMIDAZO[1,2-B]PYRIDAZINE===
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==Overview==
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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 &gt;1 microM plasma levels following a 2mg/kg oral dose to mice.
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(as it appears on PubMed at http://www.pubmed.gov), where 15081018 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15081018}}
==About this Structure==
==About this Structure==
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[[Category: Serine/threonine-protein kinase]]
[[Category: Serine/threonine-protein kinase]]
[[Category: Transferase]]
[[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 Jul 28 17:33:10 2008''

Revision as of 14:33, 28 July 2008

Image:1urw.png

Template:STRUCTURE 1urw

CDK2 IN COMPLEX WITH AN IMIDAZO[1,2-B]PYRIDAZINE

Template:ABSTRACT PUBMED 15081018

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

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