• 1
    Lindgren, M., Hällbrink, M., Prochiantz, A. & Langel, Ü. (2000) Cell-penetrating peptides. Trends Pharmacol. Sci. 21, 99103.
  • 2
    Prochiantz, A. (1996) Getting hydrophilic compounds into cells: lessons from homeopeptides. Curr. Opin. Neurobiol. 6, 629634.
  • 3
    Hawiger, J. (1997) Cellular import of functional peptides to block intracellular signaling. Curr. Opin. Immunol. 9, 189194.
  • 4
    Tung, C.H. & Stein, S. (2000) Preparation and applications of peptide-oligonucleotide conjugates. Bioconj. Chem. 11, 605618.
  • 5
    Troy, C.M., Derossi, D., Prochiantz, A., Greene, L.A. & Shelanski, M.L. (1996) Downregulation of Cu/Zn superoxide dismutase leads to cell death via the nitric oxide-peroxynitrite pathway. J. Neurosci. 16, 253261.
  • 6
    Allinquant, B., Hantraye, P., Mailleux, P., Moya, K., Bouillot, C. & Prochiantz, A. (1995) Downregulation of amyloid precursor protein inhibits neurite outgrowth in vitro. J. Cell Biol. 128, 919927.
  • 7
    Chaloin, L., Vidal, P., Lory, P., Mery, J., Lautredou, N., Divita, G. & Heitz, F. (1998) Design of carrier peptide-oligonucleotide conjugates with rapid membrane translocation and nuclearlocalization properties. Biochem. Biophys. Res. Commun. 243, 601608.
  • 8
    Morris, M.C., Vidal, P., Chaloin, L., Heitz, F. & Divita, G. (1997) A new peptide vector for efficient delivery of oligonucleotides into mammalian cells. Nucleic Acids Res. 25, 27302736.
  • 9
    Antopolsky, M., Azhayeva, E., Tengvall, U., Auriola, S., Jaaskelainen, I., Ronkko, S., Honkakoski, P., Urtti, A., Lonnberg, H. & Azhayev, A. (1999) Peptide-oligonucleotide phosphorothioate conjugates with membrane translocation and nuclear localization properties. Bioconj. Chem. 10, 598606.
  • 10
    Cutrona, G., Carpaneto, E.M., Ulivi, M., Roncella, S., Landt, O., Ferrarini, M. & Boffa, L.C. (2000) Effects in live cells of a c-myc anti-gene PNA linked to a nuclear localization signal. Nat. Biotechnol. 18, 300303.
  • 11
    Astriab, F.A., Sergueev, D.S., Fisher, M., Shaw, B.R. & Juliano, R.L. (2000) Antisense inhibition of P-glycoprotein expression using peptide-oligonucleotide conjugates. Biochem. Pharmacol. 60, 8390.
  • 12
    Bongartz, J.P., Aubertin, A.M., Milhaud, P.G. & Lebleu, B. (1994) Improved biological activity of antisense oligonucleotides conjugated to a fusogenic peptide. Nucleic Acids Res. 22, 46814688.
  • 13
    Niidome, T., Wakamatsu, M., Wada, A., Hirayama, T. & Aoyagi, H. (2000) Required structure of cationic peptide for oligonucleotide-binding and -delivering into cells. J. Pept. Sci. 6, 271279.
  • 14
    Pooga, M., Soomets, U., Hallbrink, M., Valkna, A., Saar, K., Rezaei, K., Kahl, U., Hao, J.X., Xu, X.J., WiesenfeldHallin, Z., Hokfelt, T., Bartfai, A. & Langel, U. (1998) Cell penetrating PNA constructs regulate galanin receptor levels and modify pain transmission in vivo. Nat. Biotechnol. 16, 857861.
  • 15
    Dokka, S., Toledo Velasquez, D., Shi, X., Wang, L. & Rojanasakul, Y. (1997) Cellular delivery of oligonucleotides by synthetic import peptide carrier. Pharm. Res. 14, 17591764.
  • 16
    Oehlke, J., Scheller, A., Wiesner, B., Krause, E., Beyermann, M., Klauschenz, E., Melzig, M. & Bienert, M. (1998) Cellular uptake of an alpha-helical amphipathic model peptide with the potential to deliver polar compounds into the cell interior non-endocytically. Biochim. Biophys. Acta 1414, 127139.
  • 17
    Scheller, A., Oehlke, J., Wiesner, B., Dathe, M., Krause, E., Beyermann, M., Melzig, M. & Bienert, M. (1999) Structural requirements for cellular uptake of alpha-helical amphipathic peptides. J. Pept. Sci. 5, 185194.
  • 18
    Scheller, A., Wiesner, B., Melzig, M., Bienert, M. & Oehlke, J. (2000) Evidence for an amphipathicity independent cellular uptake of amphipathic cell-penetrating peptides. Eur. J. Biochem. 267, 60436049.
  • 19
    Derossi, D., Joliot, A.H., Chassaing, G. & Prochiantz, A. (1994) The third helix of the Antennapedia homeodomain translocates through biological membranes. J. Biol. Chem. 269, 1044410450.
  • 20
    Halle, W., Mann, A., Siems, W.E. & Jentzsch, K.D. (1980) In vitro cultivation and behavior of aortic endothelium cells in a low serum culture medium. Acta Biol. Med. 39, 11651175.
  • 21
    Lorenz, D., Wiesner, B., Zipper, J., Winkler, A., Krause, E., Beyermann, M., Lindau, M. & Bienert, M. (1998) Mechanism of peptide-induced mast cell degranulation – translocation and patch-clamp studies. J. Gen. Physiol. 112, 577591.
  • 22
    Bradford, M.M. (1976) A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal. Biochem. 72, 248254.
  • 23
    Takeuchi, K., Sato, N., Kasahara, H., Funayama, N., Nagafuchi, A., Yonemura, S. & Tsukita, S. (1994) Perturbation of cell adhesion and microvilli formation by antisense oligonucleotides to ERM family members. J. Cell Biol. 125, 13711384.
  • 24
    Gao, W.Y., Storm, C., Egan, W. & Cheng, Y.C. (1993) Cellular pharmacology of phosphorothioate homooligodeoxynucleotides in human cells. Mol. Pharmacol. 43, 4550.
  • 25
    Temsamani, J., Kubert, M., Tang, J., Padmapriya, A. & Agrawal, S. (1994) Cellular uptake of oligodeoxynucleotide phosphorothioates and their analogs. Antisense Res. Dev. 4, 3542.
  • 26
    Iversen, P.L., Zhu, S., Meyer, A. & Zon, G. (1992) Cellular uptake and subcellular distribution of phosphorothioate oligonucleotides into cultured cells. Antisense Res. Dev. 2, 211222.
  • 27
    Gray, G.D., Basu, S. & Wickstrom, E. (1997) Transformed and immortalized cellular uptake of oligodeoxynucleosidephosphorothioates, 3′-alkylamino oligodeoxynucleotides, 2′-O-methyl oligoribonucleotides, oligodeoxynucleoside methylphosphonates, and peptide nucleic acids. Biochem. Pharmacol. 53, 14651476.
  • 28
    Pichon, C., Arar, K., Stewart, A.J., Dodon, M.D., Gazzolo, L., Courtoy, P.J., Mayer, R., Monsigny, M. & Roche, A.C. (1997) Intracellular routing and inhibitory activity of oligonucleopeptides containing a KDEL motif. Mol. Pharmacol. 51, 431438.
  • 29
    Marti, G., Egan, W., Noguchi, P., Zon, G., Matsukura, M. & Broder, S. (1992) Oligodeoxyribonucleotide phosphorothioate fluxes and localization in hematopoietic cells. Antisense Res. Dev. 2, 2739.
  • 30
    Alahari, S.K., DeLong, R., Fisher, M.H., Dean, N.M., Viliet, P. & Juliano, R.L. (1998) Novel chemically modified oligonucleotides provide potent inhibition of P-glycoprotein expression. J. Pharmacol. Exp. Ther. 286, 419428.
  • 31
    Hartmann, G., Krug, A., Bidlingmaier, M., Hacker, U., Eigler, A., Albrecht, R., Strasburger, C.J. & Endres, S. (1998) Spontaneous and cationic lipid-mediated uptake of antisense oligonucleotides in human monocytes and lymphocytes. J. Pharmacol. Exp. Ther. 285, 920928.
  • 32
    Bennett, C.F. (1998) Antisense oligonucleotides: is the glass half full or half empty? Biochem. Pharmacol. 55, 919.
  • 33
    Higashijima, T., Burnier, J. & Ross, E.M. (1990) Regulation of Gi and Go by mastoparan, related amphiphilic peptides, and hydrophobic amines. Mechanism and structural determinants of activity. J. Biol. Chem. 265, 1417614186.
  • 34
    Mousli, M., Hugli, T.E., Landry, Y. & Bronner, C. (1994) Peptidergic pathway in human skin and rat peritoneal mast cell activation. Immunopharmacol. 27, 111.
  • 35
    Fisher, P.J., Prendergast, F.G., Ehrhardt, M.R., Urbauer, J.L., Wand, A.J., Sedarous, S.S., McCormick, D.J. & Buckley, P.J. (1994) Calmodulin interacts with amphiphilic peptides composed of all d-amino acids. Nature 368, 651653.
  • 36
    Martoglio, B., Graf, R. & Dobberstein, B. (1997) Signal peptide fragments of preprolactin and HIV-1 p-gp160 interact with calmodulin. EMBO J. 16, 66366645.
  • 37
    Mosmann, T. (1983) Rapid colorimetric assay for cellular growth and survival: application to proliferation and cytotoxicity assays. J. Immunol. Meth. 65, 5563.