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  • Title: Dipicolylamine/Metal Complexes that Promote Direct Cell-Membrane Penetration of Octaarginine.
    Author: Kawaguchi Y, Ise S, Azuma Y, Takeuchi T, Kawano K, Le TK, Ohkanda J, Futaki S.
    Journal: Bioconjug Chem; 2019 Feb 20; 30(2):454-460. PubMed ID: 30428256.
    Abstract:
    Marked promotion of membrane permeation of a cell-penetrating peptide, octaarginine (R8), was attained by attachment to a single 2,2'-dipicolylamine moiety (DPA-R8) that forms 1:1 complexes with metal ions. Studies using giant unilamellar vesicles demonstrated that DPA targets phospholipids and enhances R8 binding to the membranes in the presence of metal ions. While DPA/Zn(II) complex has been most frequently employed for chelate formation with phosphates, Ni(II) had the most prominent effect on the membrane binding and penetration of DPA-R8. Facile cytosolic distribution of DPA-R8 was also attained in a few minutes in the presence of Ni(II). Analysis of the cellular uptake methods of DPA-R8/Ni(II) suggested the involvement of direct permeation through cell membrane without the use of endocytosis. The applicability of this system to the intracellular delivery of bioactive compounds was exemplified using a peptidomimetic farnesyltransferase inhibitor, FTI277.
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