1oiq: Difference between revisions

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==Overview==
==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.
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==
==About this Structure==
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Transferred entry: 2.7.11.1]]
[[Category: Transferred entry: 2 7.11 1]]
[[Category: Beattie, J.F.]]
[[Category: Beattie, J F.]]
[[Category: Breault, G.A.]]
[[Category: Breault, G A.]]
[[Category: Byth, K.F.]]
[[Category: Byth, K F.]]
[[Category: Culshaw, J.D.]]
[[Category: Culshaw, J D.]]
[[Category: Ellston, R.P.A.]]
[[Category: Ellston, R P.A.]]
[[Category: Green, S.]]
[[Category: Green, S.]]
[[Category: Jewsbury, P.J.]]
[[Category: Jewsbury, P J.]]
[[Category: Minshull, C.A.]]
[[Category: Minshull, C A.]]
[[Category: Norman, R.A.]]
[[Category: Norman, R A.]]
[[Category: Pauptit, R.A.]]
[[Category: Pauptit, R A.]]
[[Category: Thomas, A.P.]]
[[Category: Thomas, A P.]]
[[Category: HDU]]
[[Category: HDU]]
[[Category: atp-binding]]
[[Category: atp-binding]]
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[[Category: transferase]]
[[Category: transferase]]


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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:18:13 2008''

Revision as of 15:18, 21 February 2008

File:1oiq.gif


1oiq, resolution 2.31Å

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IMIDAZOPYRIDINES: A POTENT AND SELECTIVE CLASS OF CYCLIN-DEPENDENT KINASE INHIBITORS IDENTIFIED THROUGH STRUCTURE-BASED HYBRIDISATION

OverviewOverview

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 StructureAbout this Structure

1OIQ 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.

ReferenceReference

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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