Multi-Drug Resistance in Cancer

1. Front Matter

   Pages i-ix

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2. Multidrug Resistance in Cancer

   • Bruce C. Baguley

   Pages 1-14

3. Multidrug Resistance in Oncology and Beyond: From Imaging of Drug Efflux Pumps to Cellular Drug Targets

   • Wouter B. Nagengast, Thijs H. Oude Munnink, Eli C. F. Dijkers, Geke A. P. Hospers, Adrienne H. Brouwers, Carolien P. Schröder et al.

   Pages 15-31

4. Studying Drug Resistance Using Genetically Engineered Mouse Models for Breast Cancer

   • Sven Rottenberg, Marina Pajic, Jos Jonkers

   Pages 33-45

5. Mechanisms of Multidrug Resistance in Cancer

   • Jean-Pierre Gillet, Michael M. Gottesman

   Pages 47-76

6. Molecular Mechanisms of Drug Resistance in Single-Step and Multi-Step Drug-Selected Cancer Cells

   • Anna Maria Calcagno, Suresh V. Ambudkar

   Pages 77-93

7. Pharmacogenetics of ATP-Binding Cassette Transporters and Clinical Implications

   • Ingolf Cascorbi, Sierk Haenisch

   Pages 95-121

8. Flow Cytometric Evaluation of Multidrug Resistance Proteins

   • Adorjan Aszalos, Barbara J. Taylor

   Pages 123-139

9. Targeted Chemotherapy in Drug-Resistant Tumors, Noninvasive Imaging of P-Glycoprotein-Mediated Functional Transport in Cancer, and Emerging Role of Pgp in Neurodegenerative Diseases

   • Jothilingam Sivapackiam, Seth T. Gammon, Scott E. Harpstrite, Vijay Sharma

   Pages 141-181

10. Epigenetic Regulation of Multidrug Resistance 1 Gene Expression: Profiling CpG Methylation Status Using Bisulphite Sequencing

    • Emma K. Baker, Assam El-Osta

    Pages 183-198

11. Expression and Function of P-Glycoprotein in Normal Tissues: Effect on Pharmacokinetics

    • Frantisek Staud, Martina Ceckova, Stanislav Micuda, Petr Pavek

    Pages 199-222

12. Molecular Mechanism of ATP-Dependent Solute Transport by Multidrug Resistance-Associated Protein 1

    • Xiu-bao Chang

    Pages 223-249

13. Impact of Breast Cancer Resistance Protein on Cancer Treatment Outcomes

    • Douglas D. Ross, Takeo Nakanishi

    Pages 251-290

14. Drug Ratio-Dependent Antagonism: A New Category of Multidrug Resistance and Strategies for Its Circumvention

    • Troy O. Harasym, Barry D. Liboiron, Lawrence D. Mayer

    Pages 291-323

15. Reversing Agents for ATP-Binding Cassette Drug Transporters

    • Chow H. Lee

    Pages 325-340

16. Overcoming Multidrug Resistance in Cancer: Clinical Studies of P-Glycoprotein Inhibitors

    • Helen M. Coley

    Pages 341-358

17. Pharmacokinetic and Pharmacodynamic Implications of P-Glycoprotein Modulation

    • Jeannie M. Padowski, Gary M. Pollack

    Pages 359-384

18. Examination of CYP3A and P-Glycoprotein-Mediated Drug–Drug Interactions Using Animal Models

    • Punit H. Marathe, A. David Rodrigues

    Pages 385-403

19. Generating Inhibitors of P-Glycoprotein: Where to, Now?

    • Emily Crowley, Christopher A. McDevitt, Richard Callaghan

    Pages 405-432

20. Immunosuppressors as Multidrug Resistance Reversal Agents

    • Hamid Morjani, Claudie Madoulet

    Pages 433-446

Chemotherapy is one of the major treatment options for cancer patients; however, the efficacy of chemotherapeutic management of cancer is severely limited by multidrug resistance, in that cancer cells become simultaneously resistant to many structurally and mechanistically unrelated drugs. In the past three decades, a number of mechanisms by which cancer cells acquire multidrug resistance have been discovered. In addition, the development of agents or strategies to overcome resistance has been the subject of intense study. This book contains comprehensive and up-to-date reviews of multidrug resistance mechanisms, from over-expression of ATP-binding cassette drug transporters such as P-glycoprotein, multidrug resistance-associated proteins, and breast cancer resistance p- tein to the drug ratio-dependent antagonism and the paradigm of cancer stem cells. The book also includes strategies to overcome multidrug resistance, from the development of compounds that inhibit drug transporter function to the modulation of transporter expression. In addition, this book contains techniques for the detection and imaging of drug transporters, methods for the investigation of drug resistance in animal models, and strategies to evaluate the efficacy of resistance reversal agents. The book intends to provide a state-of-the-art collection of reviews and methods for both basic and clinician investigators who are interested in cancer multidrug resistance mechanisms and reversal strategies. Tianjin, China Jun Zhou v Contents Preface. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . v Contributors. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . ix 1 MultidrugResistance in Cancer . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 1 Bruce C. Baguley 2 Multidrug Resistance in Oncology and Beyond: From Imaging of Drug Efflux Pumps to Cellular Drug Targets . . . . . . . . . . . . . . . . . . . . . . . . . .

• ATP-binding
• Cancer stem cells
• Chemotherapy
• Drug transporter function
• P-glycoproteins
• Regulation
• Resistance reversal agents
• tissue
• antibacterial drug resistance

From the reviews:

“This book uses cancer as the focus to discuss both the mechanistic events causing multi-drug resistance and the potential ways to mitigate it. … In summary, this book provides a good overview of the development and treatment of multi-drug resistance in cancer. … each individual chapter covers a specific area in an easy-to-read manner, which should leave the reader with a better understanding of the topic.” (Nick Plant, BTS Newsletter, Issue 37, Winter, 2010)

“The topics covered in this 21-chapter volume have been provided by leading experts in the field. … The chapters are generally well written and clear. … This provides a full picture on what is going on in this exciting field. … this book offers a comprehensive survey of the fields of knowledge and research concerning cancer multi-drug resistance mechanisms and reversal strategies. In this way, it is relevant for basic and clinical investigators, for the less experienced and mature researchers … .” (Rolf W. Hartmann, ChemMedChem, Vol. 6 (3), 2011)

• College of Life Sciences, Nankai University, Tianjin, China, People's Republic

  Jun Zhou

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