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EXP001477

Paper

A specific aptamer-cell penetrating peptides complex delivered siRNA efficiently and suppressed prostate tumor growth in vivo (2016)

Peptide

3TAT-DRBD (within STD fusion protein)

Sequence: GRKKRRQRRRGSHGRKKRRQRRRGSHGRKKRRQRRRGSHAGDLSAGFFMEELNTYRQKQGVVLKYQELPNSGPPHDRRFTFQVIIDGREFPEGEGRSKKEAKNAAAKLAVEILNKEKKA

RNA

siRNA

All experiment fields

Experiment Id EXP001477
Paper A specific aptamer-cell penetrating peptides complex delivered siRNA efficiently and suppressed pros
Peptide 3TAT-DRBD (within STD fusion protein)
Delivery Success Class no
In Vivo Flag no
Uptake Confirmed yes
Label Confidence high
In Vitro Functional Effect yes
Endosomal Escape Evidence
Peptide Concentration Complex dosing: 200 pmol sur-siRNA per 5×10^5 cells; final siRNA 100–400 nM; STD used at ~4–10× siRNA molar in assembly (example 20–50 µM STD with 5 µM siRNA during prep).
Rna Concentration In vitro: 200 pmol siRNA per 5×10^5 cells (final 100–400 nM depending on volume); confocal/flow assays used 200 pmol FAM-sur-siRNA.
Mixing Ratio Theoretical assembly: A10:STD:siRNA = 4:4:1 (4 DRBD per siRNA; 1 SA per biotin-A10). Assembly example: 10 µL 5 µM sur-siRNA + 10 µL 20–50 µM STD (PBS + 10% glycerol, on ice 30 min), then +10 µL 20 µM biotin-A10 (PBS pH 7.4, 30 min).
Formulation Format A10-STD-(sur-siRNA) complex (aptamer-targeted CPP/DRBD fusion protein complex)
Formulation Components STD fusion protein (streptavidin-3TAT-DRBD) + biotinylated PSMA aptamer A10 (2'-fluoro pyrimidine-modified) + SURVIVIN siRNA (FAM/Cy7-labeled for tracking in some assays).
Size Nm
Zeta Mv
Model Scope in_vitro
Model Type in vitro
Cell Lines Or Primary Cells LNCaP (PSMA+ prostate cancer). Specificity controls: PC-3 (PSMA−), HeLa (PSMA−), HepG2 (PSMA−).
Animal Model
Administration Route
Output Type Uptake/internalization (confocal microscopy + flow cytometry of FAM/Cy7-siRNA); functional effect (SURVIVIN mRNA by RT-qPCR at 48 h, protein by western blot at 72 h); apoptosis (Annexin V/PI flow cytometry ± cisplatin).
Output Value
Output Units
Output Notes A10 provided PSMA-dependent binding to LNCaP (blocked by anti-PSMA). Complex delivered FAM-siRNA to cytoplasm with high % fluorescent cells (~99.8%), higher than A10-siRNA chimera (~39.9%). SURVIVIN knockdown and increased apoptosis vs controls were observed.
Toxicity Notes Apoptosis increased after survivin knockdown; no separate general cytotoxicity panel reported beyond apoptosis assay context.
Curation Notes