Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 59, Issue 23, Pages 10520-10529Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b00936
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Funding
- Korea Drug Development Fund [KDDF-201408-03]
- Basic Science Research Program of the National Research Foundation of Korea (NRF) [2010-0027955]
- Cancer Control, Ministry of Health and Welfare [1420390]
- Korea Evaluation Institute of Industrial Technology (KEIT) [KDDF-201408-03] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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Heparin and low molecular weight heparins (LMWHs) have been the drug of choice for the treatment or the prevention of thromboembolic disease. Different methods are employed to prepare the LMWHs that are clinically approved for the market currently. In particular, enoxaparin, which has a reducing sugar moiety at the end-site of polysaccharide, is prepared by alkaline depolymerization. Focusing on this end-site-specific activity of LMWHs, we conjugated the tetraoligomer of deoxycholic acid (TetraDOCA; TD) at the end-site of enoxaparin via nonenzymatic glycosylation reaction. The end-site-specific conjugation is important for polysaccharide drug development because of the heterogeneity of polysaccharides. This study also showed that orally active enoxaparin and tetraDOCA conjugate (EnoxaTD) had therapeutic effect on deep vein thrombosis (DVT) without bleeding in animal models. Considering the importance of end-specific conjugation, these results suggest that EnoxaTD could be a drug candidate for oral heparin development.
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