Novel strategy of drug therapy for inflammatory bowel diseases based on the combination of drug transport and intestinal immunology.

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Expression of peptide transporter PEPT1 in the large intestine of inflammatory bowel disease (IBD) patients was specifically induced in the inflammatory region. Furthermore, this expression was suggested to be stimulated by intestine-specific transcription factor CDX2. Based on the literature and molecular design methods, eight kinds of amino acid derivatives of 5-aminosalicylic acid were synthesized, which can become the substrates for PEPT1. The interaction of PEPT1 with these amino acid derivatives of 5-aminosalicylic acid will be evaluated from the view points of in vitro and in vivo.