INTEGRATION OF CELL CYCLE CONTROL PATHWAYS AND THE OPPORTUNITIES FOR TARGETING Cell Cycle Dynamics and the Challenges for CDK Targeting Paul J. Smith, Emeline Furon, and Rachel J. Errington Functional Regulation of CIP/KIP CDK Inhibitors Mong-Hong Lee and Ruiying Zhao Mouse Models to Study the In Vivo Function of Cyclin-Dependent Kinases in Normal Homeostasis and Tumor Development Marcos Malumbres, Pierre Dubus, and Sagrario Ortega Cyclin-Dependent Kinase Inhibitors and Vascular Disease Martin F. Crook and Manfred Boehm CDK INHIBITORS: TARGETS AND THEIR EVALUATION Evaluation of CDK Inhibitor Selectivity: From Affinity Chromatography to Yeast Genetics Stéphane Bach, Marc Blondel, and Laurent Meijer Development of CDK Inhibitors as Anticancer Agents: From Rational Design to CDK4-Specific Inhibition Sachin Mahale and Bhabatosh Chaudhuri Three-Dimensional Structures of Cyclin-Dependent Kinases and Their Inhibitor Complexes Ursula Schulze-Gahmen and Sung-Hou Kim CDK INHIBITORS: CHEMISTRY FOCUS Cyclin-Dependent Kinase Small Molecule Modulators for Cancer Therapy Adrian M. Senderowicz (R)-Roscovitine (CYC202, Seliciclib) Laurent Meijer, Karima Bettayeb, and Hervé Galons Development, Selectivity, and Application of Paullones, a Family of CDK Inhibitors Conrad Kunick, Thomas Lemcke, and Laurent Meijer Discovery of BMS-387032, a Potent Cyclin-Dependent Kinase Inhibitor in Clinical Development John T. Hunt Oxindole Inhibitors of Cyclin-Dependent Kinases as Antitumor Agents Philip A. Harris Indenopyrazoles as Cyclin-Dependent Kinase Inhibitors David J. Carini, Catherine R. Burton, and Steven P. Seitz Development of Indolocarbazoles as Cyclin D1/CDK4 Inhibitors Guoxin Zhu Pyrazoles as Efficient Adenine-Mimetic Heterocycles for the Discovery of CDK Inhibitors Paolo Pevarello and Anna Vulpetti Pyrazolo [3,4-d] pyrimidin-4-ones: Exploring the Structural Determinants of Potency and Selectivity in Cyclin-Dependent Kinase Inhibition Jay A. Markwalder and Steven P. Seitz THERAPEUTIC PERSPECTIVE Cyclin-Dependent Kinase Inhibitors and Combination Therapy: Experimental and Clinical Status Lloyd R. Kelland CDK Inhibitors as Anticancer Agents: Perspectives for the Future Jayalakshmi Sridhar, Nagarajan Pattabiraman, Eliot M. Rosen, and Richard G. Pestell INDEX