One of the few books to cover all aspects of cyclin-dependent kinases (CDKs), Inhibitors of Cyclin-dependent Kinases as Anti-tumor Agents provides an overview of CDKs as molecular and functional entities, their involvement in different disease processes, and their potential for pharmacological modulation. With contributions from the top international researchers in the field, the book takes a contemporary approach to study the importance of rational drug design and knowledge-based therapeutics in relation to CDKs. The first two sections of the book discuss the integration of cell cycle control pathways, opportunities for targeting, targets of inhibitors, and the evaluation of CDK inhibitors, exploring topics such as the in vivo function of CDKs in normal homeostasisand tumor development and the structural biology of CDKs. The third section examines the design, development, and chemistry of small molecule CDK inhibitors, with discussions ranging from the early-stage discovery of new chemical entities with a capacity to inhibit CDKs to late-stage compounds in clinical development. The final section assesses the current status of CDK inhibitors in clinical trials, the therapeutic deployment challenges of small molecule inhibitors, and the future development of CDK inhibitors as anticancer agents. The field of drug development is at a critical point in terms of understanding the availability, advantages, and drawbacks of CDKs as therapeutic targets for small molecules. Providing the most up-to-date, in-depth coverage available in a single volume, Inhibitors of Cyclin-dependent Kinases as Anti-tumor Agents surveys the success of the agents developed thus far, the possibility of new routes to more selective inhibitors, and the growing appreciation of critical, therapeutic issues.CD Ap O agt; * 0. LiCD FIGURE 1.1 Diagrammatic representation of the mammalian mitotic cell cycle indicating the relative expression of a GFP/cyclin B1 fluorescent reporter stably transfected and expressed into the human osteosarcoma cell line U-2OS. ... Although the deletion of the N-terminal region does not interfere with the capacity of mitotic cyclins to activate CDC2 and drive the cells into mitosis, anbsp;...
|Title||:||Inhibitors of Cyclin-dependent Kinases as Anti-tumor Agents|
|Author||:||Paul J. Smith, Eddy W. Yue|
|Publisher||:||CRC Press - 2006-10-25|