Sequence: GWTLNSAGYLLGKINLKALAALAKKIL
antisense oligonucleotide analogue (anti-TAR)
| Experiment Id | EXP001580 |
|---|---|
| Paper | Synthesis, cellular uptake and HIV-1 Tat-dependent trans-activation inhibition activity of oligonucl |
| Peptide | Transportan |
| Delivery Success Class | no |
| In Vivo Flag | no |
| Uptake Confirmed | yes |
| Label Confidence | high |
| In Vitro Functional Effect | no |
| Endosomal Escape Evidence | no |
| Peptide Concentration | 2.5 µM conjugate (free delivery; typical) |
| Rna Concentration | 2.5 µM conjugate (free delivery; typical) |
| Mixing Ratio | Covalent 1:1 peptide:oligo (disulphide) |
| Formulation Format | Disulphide-linked peptide–oligonucleotide conjugate (peptide has terminal Cys; oligo has 5' C6-thiol; 3' fluorescein label). |
| Formulation Components | Transportan–oligo B (conjugate 13) |
| Size Nm | |
| Zeta Mv | |
| Model Scope | in_vitro |
| Model Type | in vitro |
| Cell Lines Or Primary Cells | HeLa Tet-Off/Tat/luc-f/luc-R stable reporter cells (Tat-dependent HIV LTR firefly luciferase; Renilla control) |
| Animal Model | |
| Administration Route | |
| Output Type | Uptake (confocal) + reporter inhibition assay |
| Output Value | very weak uptake in HeLa; no Tat-dependent trans-activation inhibition under free delivery |
| Output Units | |
| Output Notes | Free delivery incubations (5–24 h) showed fluorescence in cytosolic vesicles; no nuclear localization and no inhibition of Tat-dependent trans-activation (firefly luciferase). Authors attribute lack of activity to endosomal entrapment / insufficient release. |
| Toxicity Notes | |
| Curation Notes |