1oit
From Proteopedia
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| - | [[Image:1oit.jpg|left|200px]]<br /><applet load="1oit" size=" | + | [[Image:1oit.jpg|left|200px]]<br /><applet load="1oit" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1oit, resolution 1.60Å" /> | caption="1oit, resolution 1.60Å" /> | ||
'''IMIDAZOPYRIDINES: A POTENT AND SELECTIVE CLASS OF CYCLIN-DEPENDENT KINASE INHIBITORS IDENTIFIED THROUGH STRUCTURE-BASED HYBRIDISATION'''<br /> | '''IMIDAZOPYRIDINES: A POTENT AND SELECTIVE CLASS OF CYCLIN-DEPENDENT KINASE INHIBITORS IDENTIFIED THROUGH STRUCTURE-BASED HYBRIDISATION'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1OIT 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 HDT as [http://en.wikipedia.org/wiki/ligand ligand]. 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=AC1:Hdt Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http:// | + | 1OIT 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=HDT:'>HDT</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. 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=AC1:Hdt+Binding+Site+For+Chain+A'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1OIT OCA]. |
==Reference== | ==Reference== | ||
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[[Category: protein kinase]] | [[Category: protein kinase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb 3 09:58:40 2008'' |
Revision as of 07:58, 3 February 2008
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IMIDAZOPYRIDINES: A POTENT AND SELECTIVE CLASS OF CYCLIN-DEPENDENT KINASE INHIBITORS IDENTIFIED THROUGH STRUCTURE-BASED HYBRIDISATION
Overview
High-throughput screening identified the imidazo[1,2-a]pyridine and, bisanilinopyrimidine series as inhibitors of the cyclin-dependent kinase, CDK4. Comparison of their experimentally-determined binding modes and, emerging structure-activity trends led to the development of potent and, selective imidazo[1,2-a]pyridine inhibitors for CDK4 and in particular, CDK2.
About this Structure
1OIT is a Single protein structure of sequence from Homo sapiens with as ligand. 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-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation., Anderson M, Beattie JF, Breault GA, Breed J, Byth KF, Culshaw JD, Ellston RP, Green S, Minshull CA, Norman RA, Pauptit RA, Stanway J, Thomas AP, Jewsbury PJ, Bioorg Med Chem Lett. 2003 Sep 15;13(18):3021-6. PMID:12941325
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