Can RNAi-mediated hsp90α knockdown in combination with 17-AAG be a therapy for glioma? (2013)
Tat48–60 / sihsp90α complex + 17-AAG
Sequence: H-GRKKRRQRRRPPQ-NH2
| Experiment Id | EXP002450 |
|---|---|
| Paper | Can RNAi-mediated hsp90α knockdown in combination with 17-AAG be a therapy for glioma? |
| Peptide | Tat48–60 / sihsp90α complex + 17-AAG |
| Delivery Success Class | no |
| In Vivo Flag | no |
| Uptake Confirmed | no |
| Label Confidence | high |
| In Vitro Functional Effect | yes |
| Endosomal Escape Evidence | |
| Peptide Concentration | Tat CPP 15–50-fold molar excess to siRNA; up to 10 µM CPP used in toxicity assays |
| Rna Concentration | 200 nM siRNA |
| Mixing Ratio | siRNA:peptide molar ratios 1:15–1:50 |
| Formulation Format | non-covalent CPP/siRNA complex (SCC) |
| Formulation Components | Tat48–60 CPP + sihsp90α |
| Size Nm | |
| Zeta Mv | |
| Model Scope | in_vitro |
| Model Type | in vitro |
| Cell Lines Or Primary Cells | U87-MG glioblastoma cells |
| Animal Model | |
| Administration Route | cell culture incubation; serum-free complexing followed by serum-supplemented medium |
| Output Type | hsp90α knockdown; Hsp90α protein reduction; Akt activity; viability |
| Output Value | SCC alone: up to ~30% hsp90α mRNA knockdown at 48 h; 84% Hsp90α protein reduction; up to 19% growth inhibition at 48 h |
| Output Units | |
| Output Notes | Functional in vitro RNAi effect was demonstrated, but no in vivo functional delivery for this row; CPP alone increased hsp90α transcript levels in GBM and should be considered a confounder for mechanistic interpretation |
| Toxicity Notes | CPP and SCC showed minimal intrinsic toxicity under selected conditions; SCC caused ~15% LDH leakage only at high 100:1 peptide/siRNA ratio; SVGp12 non-tumor cells showed minimal growth inhibition |
| Curation Notes |