1ykr

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[[Image:1ykr.gif|left|200px]]
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{{STRUCTURE_1ykr| PDB=1ykr | SCENE= }}
{{STRUCTURE_1ykr| PDB=1ykr | SCENE= }}
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'''Crystal structure of cdk2 with an aminoimidazo pyridine inhibitor'''
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===Crystal structure of cdk2 with an aminoimidazo pyridine inhibitor===
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==Overview==
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Structure-based design approach was successfully used to guide the evolution of imidazopyridine scaffold yielding new structural class of highly selective inhibitors of cyclin dependent kinases that were able to form a new interaction with an identified residue of the protein, Lys89. Compounds from this series have shown no detectable effect when tested against a representative set of other serine/threonine kinases such as GSK3beta, CAMKII, PKA, PKC-alpha,beta,epsilon,gamma. Compound 2i inhibits proliferation in HCT 116 cells in tissue culture. Synthesis, co-crystal structure of CDK2 in complex with compound 2i, and preliminary SAR study are disclosed.
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The line below this paragraph, {{ABSTRACT_PUBMED_15780638}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 15780638 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15780638}}
==About this Structure==
==About this Structure==
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[[Category: Cdk2]]
[[Category: Cdk2]]
[[Category: Cell cycle division protein kinase 2]]
[[Category: Cell cycle division protein kinase 2]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 16:26:41 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 16:48:14 2008''

Revision as of 13:48, 27 July 2008

Image:1ykr.png

Template:STRUCTURE 1ykr

Crystal structure of cdk2 with an aminoimidazo pyridine inhibitor

Template:ABSTRACT PUBMED 15780638

About this Structure

1YKR is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases., Hamdouchi C, Zhong B, Mendoza J, Collins E, Jaramillo C, De Diego JE, Robertson D, Spencer CD, Anderson BD, Watkins SA, Zhang F, Brooks HB, Bioorg Med Chem Lett. 2005 Apr 1;15(7):1943-7. PMID:15780638

Page seeded by OCA on Sun Jul 27 16:48:14 2008

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