1pye

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{{STRUCTURE_1pye| PDB=1pye | SCENE= }}
{{STRUCTURE_1pye| PDB=1pye | SCENE= }}
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'''Crystal structure of CDK2 with inhibitor'''
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===Crystal structure of CDK2 with inhibitor===
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==Overview==
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The protein kinase family represents an enormous opportunity for drug development. However, the current limitation in structural diversity of kinase inhibitors has complicated efforts to identify effective treatments of diseases that involve protein kinase signaling pathways. We have identified a new structural class of protein serine/threonine kinase inhibitors comprising an aminoimidazo[1,2-a]pyridine nucleus. In this report, we describe the first successful use of this class of aza-heterocycles to generate potent inhibitors of cyclin-dependent kinases that compete with ATP for binding to a catalytic subunit of the protein. Co-crystal structures of CDK2 in complex with lead compounds reveal a unique mode of binding. Using this knowledge, a structure-based design approach directed this chemical scaffold toward generating potent and selective CDK2 inhibitors, which selectively inhibited the CDK2-dependent phosphorylation of Rb and induced caspase-3-dependent apoptosis in HCT 116 tumor cells. The discovery of this new class of ATP-site-directed protein kinase inhibitors, aminoimidazo[1,2-a]pyridines, provides the basis for a new medicinal chemistry tool to be used in the search for effective treatments of cancer and other diseases that involve protein kinase signaling pathways.
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The line below this paragraph, {{ABSTRACT_PUBMED_14749470}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 14749470 is the PubMed ID number.
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{{ABSTRACT_PUBMED_14749470}}
==About this Structure==
==About this Structure==
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[[Category: Cdk]]
[[Category: Cdk]]
[[Category: Cyclin-dependent kinase 2]]
[[Category: Cyclin-dependent kinase 2]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 05:38:30 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 12:49:14 2008''

Revision as of 09:49, 29 July 2008

Image:1pye.png

Template:STRUCTURE 1pye

Crystal structure of CDK2 with inhibitor

Template:ABSTRACT PUBMED 14749470

About this Structure

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

Reference

The discovery of a new structural class of cyclin-dependent kinase inhibitors, aminoimidazo[1,2-a]pyridines., Hamdouchi C, Keyser H, Collins E, Jaramillo C, De Diego JE, Spencer CD, Dempsey JA, Anderson BD, Leggett T, Stamm NB, Schultz RM, Watkins SA, Cocke K, Lemke S, Burke TF, Beckmann RP, Dixon JT, Gurganus TM, Rankl NB, Houck KA, Zhang F, Vieth M, Espinosa J, Timm DE, Campbell RM, Patel BK, Brooks HB, Mol Cancer Ther. 2004 Jan;3(1):1-9. PMID:14749470

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