1. Multidrug Resistance in Cancer
Bruce C. Baguley
2. 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, Marjolijn Lub-de Hooge, and Elisabeth G.E. de Vries
3. Studying Drug Resistance Using Genetically Engineered Mouse Models for Breast Cancer
Sven Rottenberg, Marina Pajic, and Jos Jonkers
4. Mechanisms of Multidrug Resistance in Cancer
Jean-Pierre Gillet and Michael M. Gottesman
5. Molecular Mechanisms of Drug Resistance in Single-Step and Multi-Step Drug-Selected Cancer Cells
Anna Maria Calcagno and Suresh V. Ambudkar
6. Pharmacogenetics of ATP-Binding Cassette Transporters and Clinical Implications
Ingolf Cascorbi and Sierk Haenisch
7. Flow Cytometric Evaluation of Multidrug Resistance Proteins
Adorjan Aszalos and Barbara J. Taylor
8. Targeted Chemotherapy in Drug Resistant Tumors and Noninvasive Imaging of P-Glycoprotein-Mediated Functional Transport in Cancer
Jothilingam Sivapackiam, Seth T. Gammon, Scott E. Harpstrite, and Vijay Sharma
9. Epigenetic Regulation of Multidrug Resistance 1 Gene Expression: Profiling CpG Methylation Status Using Bisulphite Sequencing
Emma K. Baker and Assam El-Osta
10. Expression and Function of P-Glycoprotein in Normal Tissues: Effect on Pharmacokinetics
Frantisek Staud, Martina Ceckova, Stanislav Micuda, and Petr Pavek
11. Molecular Mechanism of ATP-Dependent Solute Transport by Multidrug Resistance-Associated Protein 1
Xiu-bao Chang
12. Impact of Breast Cancer Resistance Protein on Cancer Treatment Outcomes
Douglas D. Ross and Takeo Nakanishi
13. Drug Ratio-Dependent Antagonism: A NewCategory of Multidrug Resistance and Strategies for Its Circumvention
Troy O. Harasym, Barry D. Liboiron, and Lawrence D. Mayer
14. Reversing Agents for ATP-Binding Cassette Drug Transporters
Chow H. Lee
15. Overcoming Multidrug Resistance in Cancer: Clinical Studies of P-Glycoprotein Inhibitors
Helen M. Coley
16. Pharmacokinetic and Pharmacodynamic Implications of P-Glycoprotein Modulation
Jeannie M. Padowski and Gary M. Pollack
17. Examination of CYP3A and P-Glycoprotein-Mediated Drug-Drug Interactions Using Animal Models
Punit H. Marathe and A. David Rodrigues
18. Generating Inhibitors of P-Glycoprotein: Where to, Now?
Emily Crowley, Christopher A. McDevitt, and Richard Callaghan
19. Immunosuppressors as Multidrug Resistance Reversal Agents
Hamid Morjani and Claudie Madoulet
20. Overcoming Multidrug Resistance by RNA Interference
Alexandra Stege, Andrea Krühn, and Hermann Lage
21. Circumventing Tumor Resistance to Chemotherapy by Nanotechnology
Xing-Jie Liang, Chunying Chen, Yuliang Zhao, and Paul C. Wang

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 . . . . . . . . . . . . . . . . . . . . . . . . . .