Hydrophobic CPP/HDO conjugates: a new frontier in oligonucleotide-warheaded PROTAC delivery (2024)
Sequence: LGAQSNF
HDO (DNA/RNA heteroduplex) decoy PROTAC
| 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 |