Transporters As Drug Carriers - Structure, Function, Substrates

This reference handbook is the first to provide a comprehensive overview, systematically characterizing all known transporters involved in drug elimination and resistance. Combining recent knowledge on all known classes of drug carriers, from microbes to man, it begins with a look at human and mammalian transporters. This is followed by microbial, fungal and parasitic transporters with special attention given to transport across those physiological barriers relevant for drug uptake, distribution and excretion. As a result, this key resource lays the foundations for understanding and investigating the molecular mechanisms for multidrug resistance in cancer cells, microbial resistance to antibiotics and pharmacokinetics in general. For anyone working with antibiotics and cancer chemotherapeutics, as well as being of prime interest to biochemists and biophysicists.

Gerhard Ecker is the head of the Pharmacoinformatics Initiative at the Department of Medicinal Chemistry, University of Vienna. He studied Pharmacy at the University of Vienna (Ph.D. thesis advisors: W. Fleischhacker and C.R. Noe) and did post-doctoral work with J. Seydel in Borstel (Germany) where he started his SAR and QSAR studies on P-glycoprotein. His main scientific interests are pharmacoinformatic approaches to target drug efflux pumps, in silico screening methods for promiscuous targets, and non-linear methods in drug design. Peter Chiba is a senior scientist and lecturer at the Medical University of Vienna. He holds a doctorate in Medicine from the University of Vienna and worked at the Universities of Nijmegen (The Netherlands) and South Florida (USA) as a Fulbright scholar and post-doctoral associate. His research focuses on multidrug transport and resistance to drugs in treatment of cancer and microbial disease.

"Overall, the book is well organized and the topics are clearly and easily accessible. This book offers many strengths ...but overall is quite worthwhile." (ChemMedChem, January 2011)
"Overall, the book is a specialised text (as reflected in the price) that provides a comprehensive review of drug transporters. It would also be a welcome addition to any well stocked university library." (PJ Online, 12 November 2010)

List of Contributors.
Preface.
A Personal Foreword.
Part One: Human Transporter Families Structure, Function, Physiology.
1.The ABC Transporters: Structural Insights into Drug Transport (Robert C. Ford, Alhaji B. Kamis, Ian D. Kerr, and Richard Callaghan).
2. Biochemistry, Physiology, and Pharmacology of Nucleoside and Nucleobase Transporters (Marçal Pastor-Anglada, Miriam Molina-Arcas, Pedro Cano-Soldado, and Francisco Javier Casado).
3. Organic Anion Transporting Polypeptides (Oatps/OATPs) (Mine Yarim and Meric Koksal).
4. CNS-Transporters as Drug Targets (Klaus Gundertofte).
Part Two: Drug Transport in Microorganisms and Fungi.
5. Bacterial Multidrug Transporters: Molecular and Clinical Aspects (Olga Lomovskaya, Helen I. Zgurskaya, and Keith Bostian).
6. Membrane Transporters in Pleiotropic Drug Resistance and Stress Response in Yeast and Fungal Pathogens (Tobias Schwarzmüller, Cornelia Klein, Martin Valachovic, Walter Glaser, and Karl Kuchler).
Part Three: Structure Activity Relationship Studies on ABC Transporter.
7. QSAR Studies on ABC Transporter How to Deal with Polyspecificity (Gerhard F. Ecker).
8. Drug Transporter Pharmacophores (Sean Ekins).
Part Four: Transporters and ADME.
9. Biological Membranes and Drug Transport (Gert Fricker).
10. Transport at the Blood-Brain Barrier (Winfried Neuhaus and Christian R. Noe).
11. Bile Canalicular Transporters (Dirk R. de Waart and Ronald P.J. Oude Elferink).
12. Interplay of Drug Metabolizing Enzymes and ABC Transporter (Walter Jäger).
13. ABC Transporters From Targets to Antitargets? (Gerhard F. Ecker and Peter Chiba).
Part Five: A Systems View of Drug Transport.
14. A Systems Biology View of Drug Transporters (Sean Ekins and Dana L. Abramovitz).
15. Drug Transporters in Health and Disease (Barbara Bennani-Baïti and Christian R. Noe).
Index.
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