1oit

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[[Category: protein kinase]]
[[Category: protein kinase]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 12:19:49 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 15:55:40 2007''

Revision as of 13:50, 30 October 2007


1oit, resolution 1.60Å

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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 HDT as [ligand]. Active as [Transferred entry: 2.7.11.1], with EC number [2.7.1.37]. Structure known Active Site: AC1. 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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