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EXP001727

Paper

The nuclear concentration required for antisense oligonucleotide activity in myotonic dystrophy cells (2019)

Peptide

R9 (nona-arginine)

Sequence: Ac-RRRRRRRRR-NH2

RNA

ASO (antisense oligonucleotide; steric-blocking)

All experiment fields

Experiment Id EXP001727
Paper The nuclear concentration required for antisense oligonucleotide activity in myotonic dystrophy cell
Peptide R9 (nona-arginine)
Delivery Success Class no
In Vivo Flag no
Uptake Confirmed yes
Label Confidence high
In Vitro Functional Effect no
Endosomal Escape Evidence no
Peptide Concentration At highest tested ASO dose (1 µM), peptide-only control corresponds to 10 µM R9; polyplex peptide concentration scales with ASO (10:1 molar).
Rna Concentration ASO tested 0.1–1.0 µM (24 h incubation) for splice correction; imaging/uptake typically 0.1 µM Cy5-ASO.
Mixing Ratio N/P = 6 (R9), corresponding to peptide:ASO molar ratio 10:1; polyplexes stabilized ~1 h RT.
Formulation Format Noncovalent CPP/ASO polyplex (charge-driven nanoparticle)
Formulation Components R9 + steric-blocking ASO (CAG5) in serum-free medium; noncovalent polyplexes.
Size Nm
Zeta Mv
Model Scope in_vitro
Model Type in vitro
Cell Lines Or Primary Cells Immortalized human DM1 myoblasts (DM11 cl5) and unaffected myoblasts (C25); fibroblast validation in some experiments
Animal Model
Administration Route
Output Type in vitro splice correction (DM1 biomarkers)
Output Value No measurable splice correction of MBNL1 (exons 5/7) or DMD (exon 78) vs untreated DM1 cells across tested doses.
Output Units
Output Notes 24 h treatment + 24 h recovery; RT-PCR quantification of exon inclusion. Confocal/FLIM indicate mostly vesicular/mitochondrial Cy5 signal with degradation; no homogeneous nuclear ASO distribution observed.
Toxicity Notes Not the focus for R9; higher PF14 doses showed reduced viability; R9 peptide-only control included.
Curation Notes