2f2c

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{{STRUCTURE_2f2c| PDB=2f2c | SCENE= }}
{{STRUCTURE_2f2c| PDB=2f2c | SCENE= }}
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'''X-ray structure of human CDK6-Vcyclinwith the inhibitor aminopurvalanol'''
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===X-ray structure of human CDK6-Vcyclinwith the inhibitor aminopurvalanol===
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==Overview==
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Cyclin-dependent kinases (CDKs) are key players in cell cycle control, and genetic alterations of CDKs and their regulators have been linked to a variety of cancers. Hence, CDKs are obvious targets for therapeutic intervention in various proliferative diseases, including cancer. To date, drug design efforts have mostly focused on CDK2 because methods for crystallization of its inhibitor complexes have been well established. CDK4 and CDK6, however, may be at least as important as enzymes for cell cycle regulation and could provide alternative treatment options. We describe here two complex structures of human CDK6 with a very specific kinase inhibitor, PD0332991, which is based on a pyrido[2,3-d]pyrimidin-7-one scaffold, and with the less specific aminopurvalanol inhibitor. Analysis of the structures suggests that relatively small conformational differences between CDK2 and CDK6 in the hinge region are contributing to the inhibitor specificity by inducing changes in the inhibitor orientation that lead to sterical clashes in CDK2 but not CDK6. These complex structures provide valuable insights for the future development of CDK-specific inhibitors.
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The line below this paragraph, {{ABSTRACT_PUBMED_16789739}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16789739 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16789739}}
==About this Structure==
==About this Structure==
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[[Category: Schulze-Gahmen, U]]
[[Category: Schulze-Gahmen, U]]
[[Category: Small molecule inhibitor bound between n-terminal and c-terminal domain of kinase]]
[[Category: Small molecule inhibitor bound between n-terminal and c-terminal domain of kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 03:22:55 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 20:17:03 2008''

Revision as of 17:17, 28 July 2008

Image:2f2c.png

Template:STRUCTURE 2f2c

X-ray structure of human CDK6-Vcyclinwith the inhibitor aminopurvalanol

Template:ABSTRACT PUBMED 16789739

About this Structure

2F2C is a Protein complex structure of sequences from Homo sapiens and Saimiriine herpesvirus 2. Full crystallographic information is available from OCA.

Reference

Toward understanding the structural basis of cyclin-dependent kinase 6 specific inhibition., Lu H, Schulze-Gahmen U, J Med Chem. 2006 Jun 29;49(13):3826-31. PMID:16789739

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