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EXP001478

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 EXP001478
Paper A specific aptamer-cell penetrating peptides complex delivered siRNA efficiently and suppressed pros
Peptide 3TAT-DRBD (within STD fusion protein)
Delivery Success Class yes
In Vivo Flag yes
Uptake Confirmed no
Label Confidence high
In Vitro Functional Effect
Endosomal Escape Evidence
Peptide Concentration Systemic dosing described by siRNA amount: 400 pmol sur-siRNA per tail-vein injection, every other day ×7 (STD and A10 assembled as complex).
Rna Concentration In vivo: 400 pmol sur-siRNA per injection (tail vein).
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_vivo
Model Type in vivo
Cell Lines Or Primary Cells
Animal Model Male athymic BALB/c nude mice bearing LNCaP (PSMA+) subcutaneous xenografts (controls: PC-3 and HeLa xenografts for specificity imaging).
Administration Route Intravenous (tail/caudal vein) systemic administration
Output Type In vivo efficacy: tumor growth suppression (tumor volume over 21 days; tumor weight at day 21) after systemic dosing; in vivo targeting by Cy7 fluorescence imaging (IVIS) at 24 h post-injection.
Output Value
Output Units
Output Notes After systemic administration, complex significantly suppressed LNCaP xenograft growth versus free siRNA and comparators; Cy7 imaging showed preferential accumulation in PSMA+ LNCaP xenografts (aptamer-dependent).
Toxicity Notes Two accidental deaths reported in complex group during study (days ~13–15); no full PK/toxicity profiling included.
Curation Notes