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Membrane Transporters: Structure, Function and Targets for Drug Design

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Transporters as Targets for Drugs

Part of the book series: Topics in Medicinal Chemistry ((TMC,volume 4))

Abstract

Current therapeutic drugs act on four main types of molecular targets: enzymes, receptors, ion channelsand transporters, among which a major part (60–70%) are membrane proteins. This review discussesthe molecular structures and potential impact of membrane transporter proteins on new drug discovery. Thethree-dimensional (3D) molecular structure of a protein contains information about the active siteand possible ligand binding, and about evolutionary relationships within the protein family. Transportershave a recognition site for a particular substrate, which may be used as a target for drugsinhibiting the transporter or acting as a false substrate. Three groups of transporters have particularinterest as drug targets: the major facilitator superfamily, which includes almost 4000 different proteinstransporting sugars, polyols, drugs, neurotransmitters, metabolites, amino acids, peptides, organic andinorganic anions and many other substrates; the ATP-binding cassette superfamily, which plays an importantrole in multidrug resistance in cancer chemotherapy; and the neurotransmitter:sodium symporter family, whichincludes the molecular targets for some of the most widely used psychotropic drugs. Recent technical advanceshave increased the number of known 3D structures of membrane transporters, and demonstrated that they forma divergent group of proteins with large conformational flexibility which facilitates transport ofthe substrate.

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Authors and Affiliations

  1. Department of Pharmacology, Institute of Medical Biology, Faculty of Medicine, University of Tromsø, 9037, Tromsø, Norway

    Aina W. Ravna, Georg Sager, Svein G. Dahl & Ingebrigt Sylte

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  1. Aina W. Ravna
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  2. Georg Sager
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  3. Svein G. Dahl
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  4. Ingebrigt Sylte
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Correspondence to Ingebrigt Sylte .

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Susan Napier Matilda Bingham

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Ravna, A.W., Sager, G., Dahl, S.G., Sylte, I. (2008). Membrane Transporters: Structure, Function and Targets for Drug Design. In: Napier, S., Bingham, M. (eds) Transporters as Targets for Drugs. Topics in Medicinal Chemistry, vol 4. Springer, Berlin, Heidelberg. https://doi.org/10.1007/7355_2008_023

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