Sequence: GRKKRRQRRRP
antisense oligonucleotide analogue (anti-TAR)
| Experiment Id | EXP001576 |
|---|---|
| Paper | Synthesis, cellular uptake and HIV-1 Tat-dependent trans-activation inhibition activity of oligonucl |
| Peptide | Tat (48–58) |
| Delivery Success Class | no |
| In Vivo Flag | no |
| Uptake Confirmed | yes |
| Label Confidence | high |
| In Vitro Functional Effect | yes |
| Endosomal Escape Evidence | yes |
| Peptide Concentration | Dose range tested (≤1 µM typical) delivered with Lipofectamine 2000 (3 h) |
| Rna Concentration | Dose range tested (≤1 µM typical) delivered with Lipofectamine 2000 (3 h) |
| Mixing Ratio | Covalent 1:1 peptide:oligo (disulphide) + cationic lipid formulation |
| Formulation Format | peptide–oligo conjugate formulated with cationic lipid (Lipofectamine 2000) |
| Formulation Components | Tat–oligo B (C-terminal Tat conjugate; conjugate 4) + Lipofectamine 2000 |
| 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 | Functional steric-block activity (Tat-dependent firefly luciferase inhibition) |
| Output Value | Dose-dependent inhibition of firefly luciferase (Tat-dependent trans-activation) with minimal Renilla effect (specific) |
| Output Units | |
| Output Notes | With cationic lipid (Lipofectamine 2000), certain conjugates showed dose-dependent inhibition of firefly luciferase (Tat-dependent trans-activation) with minimal effect on Renilla for active conjugates. |
| Toxicity Notes | Viability (CellTiter) used for normalization in reporter assay. |
| Curation Notes |