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Transporters as Drug Carriers. Structure, Function, Substrates. Methods and Principles in Medicinal Chemistry

  • ID: 2183125
  • Book
  • 449 Pages
  • John Wiley and Sons Ltd
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Administering a drug specifically to where it is intended to act is no easy task, since all organisms have evolved highly efficient mechanisms to rid themselves of unwanted, ′foreign′ molecules. Knowledge about the abundance and specificity of the transporter molecules mediating the drug elimination can thus make the difference between ineffective and successful drug therapy. This is why the action of drug transporters is a key concern in antimicrobial therapy, cancer and many other diseases targeted by drugs.

This is the first reference handbook to provide a comprehensive overview of the topic, 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.

The result is a key resource that lays the foundations for understanding and investigating the molecular mechanisms for multidrug resistance in cancer cells, microbial resistance to antibiotics and pharmacokinetics in general.
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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


5 Bacterial Multidrug Transporters: Molecular and Clinical Aspects

6 Pleiotropic drug resistance in yeast and fungal pathogens


7 QSAR studies on ABC–transporters: how to deal with polyspecificity

8 Drug Transporter Pharmacophores


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


14 A Systems Biology View of Drug Transporters

15 Drug Transporters in Health and Disease

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Gerhard F. Ecker
Peter Chiba
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