VLDL/LDL acts as a drug carrier and regulates the transport and metabolism of drugs in the body View Full Text


Ontology type: schema:ScholarlyArticle      Open Access: True


Article Info

DATE

2017-04-04

AUTHORS

Hideaki Yamamoto, Tappei Takada, Yoshihide Yamanashi, Masatsune Ogura, Yusuke Masuo, Mariko Harada-Shiba, Hiroshi Suzuki

ABSTRACT

Only free drugs have been believed to be carried into tissues through active or passive transport. However, considering that lipoproteins function as carriers of serum lipids such as cholesterol and triglycerides, we hypothesized that lipoproteins can associate with certain drugs and mediate their transport into tissues in lipid-associated form. Here, in vitro and in vivo studies with low density lipoprotein receptor (LDLR)-overexpressing or -knockdown cells and wild-type or LDLR-mutant mice were used to show the association of various drugs with lipoproteins and the uptake of lipoprotein-associated drugs through a lipoprotein receptor-mediated process. In clinical studies, investigation of the effect of lipoprotein apheresis on serum drug concentrations in patients with familial hypercholesterolemia demonstrated that lipoprotein-mediated drug transport occurs in humans as well as in mice. These findings represent a new concept regarding the transport and metabolism of drugs in the body and suggest that the role of lipoprotein-mediated drug transport should be considered when developing effective and safe pharmacotherapies. More... »

PAGES

633

References to SciGraph publications

  • 2011-08-05. BDDCS Applied to Over 900 Drugs in THE AAPS JOURNAL
  • Identifiers

    URI

    http://scigraph.springernature.com/pub.10.1038/s41598-017-00685-9

    DOI

    http://dx.doi.org/10.1038/s41598-017-00685-9

    DIMENSIONS

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    PUBMED

    https://www.ncbi.nlm.nih.gov/pubmed/28377633


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