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.

PART 1 1 The ABC Transporters: Structural Insights into Drug Transport 2 Biochemistry, Physiology, and Pharmacology of Nucleoside and Nucleobase Transporters 3 Organic Anion Transporting Polypeptides (Oatps/OATPs) 4 CNS Transporters as Drug Targets PART 2 5 Bacterial Multidrug Transporters: Molecular and Clinical Aspects 6 Pleiotropic drug resistance in yeast and fungal pathogens PART 3 7 QSAR studies on ABC-transporters: how to deal with polyspecificity 8 Drug Transporter Pharmacophores PART 4 9 Biological Membranes and Drug Transport 10 Transport at the Blood-Brain Barrier 11 Bile canalicular transporters 12 Interplay of Cytochrome P450 Isoenzymes and ABC-transporter 13 ABC-Transporter: From target to antitarget PART 3 14 A Systems Biology View of Drug Transporters 15 Drug Transporters in Health and Disease