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• W2000254449 abstract "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<mml:math xmlns:mml=http://www.w3.org/1998/Math/MathML><mml:mrow><mml:mtext>I</mml:mtext><mml:mrow><mml:mn>124</mml:mn></mml:mrow></mml:mrow></mml:math>-labeled small molecule Cdk4 inhibitors (8-cyclopentyl-6-iodo-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-<mml:math xmlns:mml=http://www.w3.org/1998/Math/MathML><mml:mi>d</mml:mi></mml:math>]-pyrimidin-7-one (CKIA) and 8-cyclopentyl-6-iodo-5-methyl-2-(5-(piperazin-1-yl)-pyridin-2-yl-amino)-8H-pyrido[2,3-<mml:math xmlns:mml=http://www.w3.org/1998/Math/MathML><mml:mi>d</mml:mi></mml:math>]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<mml:math xmlns:mml=http://www.w3.org/1998/Math/MathML><mml:mrow><mml:mrow><mml:mo>[</mml:mo><mml:mrow><mml:mtext>I</mml:mtext><mml:mrow><mml:mn>124</mml:mn></mml:mrow></mml:mrow><mml:mo>]</mml:mo></mml:mrow></mml:mrow></mml:math>CKIA and<mml:math xmlns:mml=http://www.w3.org/1998/Math/MathML><mml:mrow><mml:mrow><mml:mo>[</mml:mo><mml:mrow><mml:mtext>I</mml:mtext><mml:mrow><mml:mn>124</mml:mn></mml:mrow></mml:mrow><mml:mo>]</mml:mo></mml:mrow></mml:mrow></mml:math>CKIB observed in human tumor cells are promising prerequisites for in vivo biodistribution and imaging studies." @default.
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• W2000254449 date "2009-01-01" @default.
• W2000254449 modified "2023-09-25" @default.
• W2000254449 title "Cell Cycle Regulating Kinase Cdk4 as a Potential Target for Tumor Cell Treatment and Tumor Imaging" @default.
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• W2000254449 doi "https://doi.org/10.1155/2009/106378" @default.
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