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Cell Cycle Regulating Kinase Cdk4 as a Potential Target for Tumor Cell Treatment and Tumor Imaging
Joint Authors
Mosch, Birgit
Graf, Franziska
Koehler, Lena
Pietzsch, Jens
Kniess, Torsten
Wuest, Frank
Source
Issue
Vol. 2009, Issue 2009 (31 Dec. 2009), pp.1-12, 12 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2009-06-17
Country of Publication
Egypt
No. of Pages
12
Main Subjects
Abstract EN
The cyclin-dependent kinase (Cdk)-cyclin D/retinoblastoma (pRb)/E2F cascade, which controls the G1/S transition of cell cycle, has been found to be altered in many neoplasias.
Inhibition of this pathway by using, for example, selective Cdk4 inhibitors has been suggested to be a promising approach for cancer therapy.
We hypothesized that appropriately radiolabeled Cdk4 inhibitors are suitable probes for tumor imaging and may be helpful studying cell proliferation processes in vivo by positron emission tomography.
Herein, we report the synthesis and biological, biochemical, and radiopharmacological characterizations of two I124-labeled small molecule Cdk4 inhibitors (8-cyclopentyl-6-iodo-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]-pyrimidin-7-one (CKIA) and 8-cyclopentyl-6-iodo-5-methyl-2-(5-(piperazin-1-yl)-pyridin-2-yl-amino)-8H-pyrido[2,3-d]pyrimidin-7-one (CKIB)).
Our data demonstrate a defined and specific inhibition of tumor cell proliferation through CKIA and CKIB by inhibition of the Cdk4/pRb/E2F pathway emphasizing potential therapeutic benefit of CKIA and CKIB.
Furthermore, radiopharmacological properties of [I124]CKIA and [I124]CKIB observed in human tumor cells are promising prerequisites for in vivo biodistribution and imaging studies.
American Psychological Association (APA)
Graf, Franziska& Koehler, Lena& Kniess, Torsten& Wuest, Frank& Mosch, Birgit& Pietzsch, Jens. 2009. Cell Cycle Regulating Kinase Cdk4 as a Potential Target for Tumor Cell Treatment and Tumor Imaging. Journal of Oncology،Vol. 2009, no. 2009, pp.1-12.
https://search.emarefa.net/detail/BIM-446864
Modern Language Association (MLA)
Graf, Franziska…[et al.]. Cell Cycle Regulating Kinase Cdk4 as a Potential Target for Tumor Cell Treatment and Tumor Imaging. Journal of Oncology No. 2009 (2009), pp.1-12.
https://search.emarefa.net/detail/BIM-446864
American Medical Association (AMA)
Graf, Franziska& Koehler, Lena& Kniess, Torsten& Wuest, Frank& Mosch, Birgit& Pietzsch, Jens. Cell Cycle Regulating Kinase Cdk4 as a Potential Target for Tumor Cell Treatment and Tumor Imaging. Journal of Oncology. 2009. Vol. 2009, no. 2009, pp.1-12.
https://search.emarefa.net/detail/BIM-446864
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-446864