Translocation properties of novel cell penetrating transportan and penetratin analogues.
Novel analogues of the cell-penetrating peptides penetratin and transportan were synthesized. The distribution of the biotin-labeled peptides in Bowes melanoma cell line has been investigated by indirect fluorescence with fluorescein-streptavidin detection. The time course of uptake of (125)I-labeled transportan analogues has been characterized in the same cell line. Molecular modeling was used to analyze the penetration and the orientation of molecules in a simulated biological membrane. The results, both from molecular modeling and fluorescence studies, imply that penetratin and transportan do not enter the cells by related mechanisms and that they do not belong to the same family of translocating peptides.
Lindgren
M
M
Department of Neurochemistry and Neurotoxicology, Arrhenius Laboratories, Stockholm University, S-106 91 Stockholm, Sweden.
Gallet
X
X
Soomets
U
U
Hällbrink
M
M
Bråkenhielm
E
E
Pooga
M
M
Brasseur
R
R
Langel
U
U
D000595:Amino Acid Sequence; D002352:Carrier Proteins / Q000138:chemical synthesis* / Q000378:metabolism; D002462:Cell Membrane / Q000378:metabolism; D057846:Cell-Penetrating Peptides; D004337:Drug Carriers; D019004:Galanin; D006801:Humans; D008545:Melanoma; D008958:Models, Molecular; D008969:Molecular Sequence Data; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics*; D011487:Protein Conformation; D011993:Recombinant Fusion Proteins / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D014407:Tumor Cells, Cultured; D014862:Wasp Venoms
D002352:Carrier Proteins; D057846:Cell-Penetrating Peptides; D004337:Drug Carriers; D010455:Peptides; D011993:Recombinant Fusion Proteins; D014862:Wasp Venoms; C110068:transportan; D019004:Galanin; C414409:penetratin