Inhibitors of Cyclin-dependent Kinases as Anti-tumor Agents: 1st Edition (Hardback) book cover

Inhibitors of Cyclin-dependent Kinases as Anti-tumor Agents

1st Edition

Edited by Paul J. Smith, Eddy W. Yue

CRC Press

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Hardback: 9780849337741
pub: 2006-10-25
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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.


"Smith and Yue have done an admirable job with this volume. There is a clear logic in the arrangement of the chapters. The introductory chapter is well suited to readers who are not familiar with this particular topic. Jargon is kept to a bar minimum . . . This highly readable volume should serve to get newcomers to the field up to speed quite quickly."

– D. Eric Walters, Department of Biochemistry and Molecular Biology, Rosalind Franklin University of Medicine, in Journal of Medicinal Chemistry, 2007, Vol. 50, No. 19

"Providing up-to-date, in-depth coverage 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."

– In Anticancer Research, Sept/ Oct 2007, Vol. 27, No. 5A

Table of Contents


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


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


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


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


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Subject Categories

BISAC Subject Codes/Headings:
MEDICAL / Biochemistry
MEDICAL / Pharmacology
SCIENCE / Chemistry / General