Elucidating the molecular mechanism of drug transport through structural studies of peptide transport proteins.

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The design of drugs for oral administration is common practice in the pharmaceutical industry due to ease of patient administration, storage, distribution and patient compliance. Many drugs however are poorly absorbed in the gastrointestinal (GI) tract, the main route by which orally administered drugs enter the blood stream. One successful approach to overcome this obstacle has been the design of prodrugs. Prodrugs are modified drug compounds that target nutrient transporters in the GI tract. Of these, oligopeptide transporters are the most promising targets as they are highly expressed in the GI tract and are already responsible for the uptake of antibiotics. This prodrug strategy has already been successful in improving the oral bioavailability of a number of medically important antivirals. The role of this research proposal is to gain an understanding of the underlying mechanism by which these peptide transporters function. Such information will enable a more rational extension of the initial prodrug approach with benefits for both patients and the pharmaceutical industry alike.