Carrier-mediated cellular uptake of pharmaceutical drugs: An exception or the rule?

Paul D. Dobson, Douglas B. Kell

    Research output: Contribution to journalArticlepeer-review

    Abstract

    It is generally thought that many drug molecules are transported across biological membranes via passive diffusion at a rate related to their lipophilicity. However, the types of biophysical forces involved in the interaction of drugs with lipid membranes are no different from those involved in their interaction with proteins, and so arguments based on lipophilicity could also be applied to drug uptake by membrane transporters or carriers. In this article, we discuss the evidence supporting the idea that rather than being an exception, carrier-mediated and active uptake of drugs may be more common than is usually assumed - including a summary of specific cases in which drugs are known to be taken up into cells via defined carriers - and consider the implications for drug discovery and development.
    Original languageEnglish
    Pages (from-to)205-220
    Number of pages15
    JournalNature Reviews Drug Discovery
    Volume7
    Issue number3
    DOIs
    Publication statusPublished - Mar 2008

    Keywords

    • BLOOD-BRAIN-BARRIER
    • ANION-TRANSPORTING POLYPEPTIDE
    • ORGANIC CATION
    • TRANSPORTER
    • LIPID-BILAYER-MEMBRANES
    • CENTRAL-NERVOUS-SYSTEM
    • HUMAN
    • INTESTINAL-ABSORPTION
    • BIOCHEMICAL NETWORK MODELS
    • BETA-LACTAM
    • ANTIBIOTICS
    • PH-DEPENDENT TRANSPORT
    • HUMAN PROTEIN ATLAS

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