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EXP001041

Paper

Hydrophobic CPP/HDO conjugates: a new frontier in oligonucleotide-warheaded PROTAC delivery (2024)

Peptide

P4

Sequence: LGAQSNF

RNA

HDO (DNA/RNA heteroduplex) decoy PROTAC

All experiment fields

Experiment Id EXP001041
Paper Hydrophobic CPP/HDO conjugates: a new frontier in oligonucleotide-warheaded PROTAC delivery
Peptide P4
Delivery Success Class no
In Vivo Flag no
Uptake Confirmed yes
Label Confidence high
In Vitro Functional Effect yes
Endosomal Escape Evidence no
Peptide Concentration 1–10 µM tested; ERα degradation at 10 µM (24 h, no transfection)
Rna Concentration 1–10 µM (same as peptide-conjugate dose; treated as CPP/HDO-PROTAC)
Mixing Ratio 1:1 (LCL-HDO-F : P4-HDO-R; annealed duplex)
Formulation Format annealed duplex; covalent P4 conjugation to antisense strand (P4-HDO-R, click chemistry)
Formulation Components CPP/HDO-PROTAC = LCL-HDO-F (5′-LCL-GTCAGGTCACAGTGACCTGATCAAAGTTAA-3′) + P4-HDO-R (3′-CAGTCCAGTGTCACTGGACTAguuucaa uu-5′-P4)
Size Nm
Zeta Mv
Model Scope in_vitro
Model Type in vitro
Cell Lines Or Primary Cells MCF-7 (human breast cancer cells; ERα-positive)
Animal Model
Administration Route
Output Type ERα degradation; proliferation inhibition; uptake imaging
Output Value ERα degradation at 10 µM after 24 h (no transfection); growth inhibition at 1–10 µM after 72 h; brighter cellular fluorescence vs FAM-HDOdna after 2 h
Output Units
Output Notes Fluorescence microscopy: after 2 h, punctate fluorescence co-localized with LysoTracker Red, indicating most internalized decoys remained within endosomes/lysosomes (endosomal entrapment).
Toxicity Notes Cell proliferation assessed by WST-8 viability assay (no explicit toxicity statement reported).
Curation Notes