title: Lipid-anchored drugs for delivery into subcellular compartments.
abstract: Bioavailability is a quantitative measure of the capacity of a drug to reach systemic circulation. However, if a drug target is localized in a subcellular organelle, then the drug may not be able to reach it and the effect of the drug will not be attained. Although most drug targets are localized within intracellular compartments, specific targeting of drugs at the subcellular level is not well established. Membrane proteins, lipids, nutrients and some pathogens are internalized into the cell to be targeted to distinct subcellular compartments via membrane trafficking. Recent advances have identified novel methods of subcellular drug targeting, involving the use of conjugation to ligands of cell surface receptors or to lipid anchors. In this review, we focus on the importance of subcellular targeting of drugs, in particular, the mechanism of lipid-anchoring as a novel strategy and its potential application for the treatment of several diseases.
authors.affiliation: Systems and Cell Biology of Neurodegeneration, Psychiatry Research, University of Zurich, August-Forel Strasse 1, 8008 Zurich, Switzerland. rajendran@bli.uzh.ch
authors.forename: Lawrence
authors.initials: L
authors.lastname: Rajendran
authors.forename: Vinod
authors.initials: V
authors.lastname: Udayar
authors.forename: Zoë V
authors.initials: ZV
authors.lastname: Goodger
mesh_terms: D000818:Animals; D016503:Drug Delivery Systems / Q000379:methods; D006801:Humans; D042541:Intracellular Space / Q000378:metabolism*; D008055:Lipids / Q000008:administration & dosage* / Q000737:chemistry; D026901:Membrane Transport Proteins / Q000378:metabolism*; D004364:Pharmaceutical Preparations / Q000008:administration & dosage*; D011956:Receptors, Cell Surface / Q000378:metabolism*
chemical_list: D008055:Lipids; D026901:Membrane Transport Proteins; D004364:Pharmaceutical Preparations; D011956:Receptors, Cell Surface