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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Cyclin-Dependent Kinase 4/6 (Cdk4/6) Inhibitors: Perspectives in Cancer Therapy and Imaging

Author(s): F. Graf, B. Mosch, L. Koehler, R. Bergmann, F. Wuest and J. Pietzsch

Volume 10, Issue 6, 2010

Page: [527 - 539] Pages: 13

DOI: 10.2174/138955710791384072

Price: $65


Cyclin-dependent kinases 4 and 6 (Cdk4/6) are important components of cell cycle activation and control in early G1 phase. Both enzymes and their regulators, e.g., cyclins, play critical roles in embryogenesis, homeostasis, and cancerogenesis. Cdk4/6 are attractive targets for cancer treatment. Recently, numerous selective small molecule inhibitors of Cdk4/6 have been developed. The potential of Cdk4/6 inhibitors, particularly, pyrido[2,3-d]pyrimidine derivatives, as both anti-cancer drugs and 124I- and 18F-radiolabeled tracers for cancer imaging using positron emission tomography is discussed.

Keywords: Cell cycle regulation, pyrido[2,3-d]pyrimidine, iodine-124, fluorine-18, radiolabeling, positron emission tomography

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