Youngro Byun1,2 and Taslim Al-Hilal1
1Department of Molecular Medicine and Biopharmaceutical Science, Seoul National University, Seoul 153-741, Republic of Korea
2College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea
We describe the development of apical sodium-dependent bile acid transporter (ASBT)-targeted high-affinity oligomeric bile acid substrates that mediate the transmembrane transport of low molecular weight heparin (LMWH). The conjugated tetraDOCA interacted with several hydrophobic grooves in the substrate-binding pocket of ASBT. Orally absorbed LHe-tetraD successfully prevented thrombosis in a rat model of deep vein thrombosis.