Document Detail

Whether to target single or multiple CDKs for therapy? That is the question.
MedLine Citation:
PMID:  20836132     Owner:  NLM     Status:  MEDLINE    
Complexes consisting of cyclin-dependent kinases (CDKs) and their regulatory subunits (the cyclins) control the progression of normal mammalian cells through the cell cycle. However, during malignant transformation this regulatory apparatus malfunctions, allowing cells to undergo unchecked proliferation. In many cases, the high mitotic potential of malignant cells is due to the constitutive activation of CDK-cyclin complexes, facilitated by the inactivation of cellular CDK inhibitors, such as p16(INK4A) or p27(Kip1), and the loss of functional tumor suppressors, such as the p53 and pRb proteins. It has recently been suggested that pharmacological intervention based on remedying the deficiency or loss of activity of these negative regulators of the cell cycle could be a very effective therapeutic option in the treatment of cancer. Multiple CDK inhibitors have been synthesized over the last two decades, spanning at least five classes of compounds. While these inhibitors can be classified on the basis of their chemical structure, it may be more interesting to categorize them according to their pharmacological nature, as broad-spectrum unspecific, pan-specific, or very selective antagonists. This review offers a critical assessment of the advantages and disadvantages of both pan-specific and highly selective CDK inhibitors in therapy.
Józefa Węsierska-Gądek; Margarita Maurer; Nora Zulehner; Oxana Komina
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of cellular physiology     Volume:  226     ISSN:  1097-4652     ISO Abbreviation:  J. Cell. Physiol.     Publication Date:  2011 Feb 
Date Detail:
Created Date:  2010-11-30     Completed Date:  2011-01-06     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0050222     Medline TA:  J Cell Physiol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  341-9     Citation Subset:  IM    
Copyright Information:
© 2010 Wiley-Liss, Inc.
Cell Cycle Regulation Group, Div., Department of Medicine I, Institute of Cancer Research, Medical University of Vienna, Vienna, Austria.
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MeSH Terms
Cell Cycle / physiology
Clinical Trials as Topic
Cyclin-Dependent Kinase Inhibitor Proteins / metabolism,  therapeutic use
Cyclin-Dependent Kinases* / antagonists & inhibitors,  metabolism
Cyclins / metabolism*
Enzyme Activation
Molecular Structure
Neoplasms* / drug therapy,  metabolism
Protein Kinase Inhibitors / chemistry,  therapeutic use*
Protein Subunits / metabolism
Tumor Suppressor Proteins / metabolism
Reg. No./Substance:
0/Cyclin-Dependent Kinase Inhibitor Proteins; 0/Cyclins; 0/Protein Kinase Inhibitors; 0/Protein Subunits; 0/Tumor Suppressor Proteins; EC Kinases

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