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 | EXP002452 |
|---|---|
| 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 | yes |
| In Vivo Flag | yes |
| Uptake Confirmed | no |
| Label Confidence | medium |
| In Vitro Functional Effect | |
| Endosomal Escape Evidence | |
| Peptide Concentration | Tat CPP 50-fold molar excess to siRNA |
| Rna Concentration | SCC 5 mg/kg; siRNA stock 0.5 mM; 17-AAG 80 mg/kg |
| Mixing Ratio | 50-fold peptide molar excess |
| Formulation Format | non-covalent CPP/siRNA complex plus 17-AAG |
| Formulation Components | Tat48–60 CPP + sihsp90α + mannitol + 17-AAG |
| Size Nm | |
| Zeta Mv | |
| Model Scope | in_vivo |
| Model Type | in vivo |
| Cell Lines Or Primary Cells | |
| Animal Model | U87-MG-luc2 intracranial glioblastoma xenograft in homozygous female nude mice |
| Administration Route | tail-vein injection of SCC; intraperitoneal 17-AAG |
| Output Type | hsp90α knockdown and Akt activity attenuation in tumor tissue |
| Output Value | Preliminary in vivo study: 73% hsp90α knockdown and 75% Akt activity reduction at 24 h after combination treatment |
| Output Units | |
| Output Notes | delivery_success_class = 1 because functional in vivo RNAi target knockdown was reported; confidence set to medium because animal numbers were limited (control n=1, treated n=3) and effect was measured at 24 h rather than survival/tumor-size endpoint |
| Toxicity Notes | In vivo toxicity not extensively characterized in this paper; in vitro CPP/SCC toxicity was minimal at selected doses |
| Curation Notes |