Sequence: GWTLNSAGYLLGKINLKALAALAKKIL
PNA (peptide nucleic acid; antisense)
| Experiment Id | EXP001759 |
|---|---|
| Paper | Cell penetrating PNA constructs regulate galanin receptor levels and modify pain transmission in viv |
| Peptide | Transportan |
| Delivery Success Class | no |
| In Vivo Flag | no |
| Uptake Confirmed | yes |
| Label Confidence | high |
| In Vitro Functional Effect | yes |
| Endosomal Escape Evidence | |
| Peptide Concentration | 0.1–3 µM construct for binding assays (36 h); imaging used 1 µM for 4 h; biotinyl-transportan 10 µM 30 min |
| Rna Concentration | 0.1–3 µM construct for binding assays (36 h); imaging used 1 µM for 4 h; biotinyl-transportan 10 µM 30 min |
| Mixing Ratio | |
| Formulation Format | Covalent CPP–PNA conjugate (disulfide-linked) |
| Formulation Components | Carrier peptide (transportan or pAntp/penetratin) linked to cysteine-extended 21-mer PNA via disulfide bond; intracellular reduction releases PNA. |
| Size Nm | |
| Zeta Mv | |
| Model Scope | in_vitro |
| Model Type | in vitro |
| Cell Lines Or Primary Cells | Bowes melanoma cells (human); Rin m5F (rat insulinoma) mentioned for receptor half-life estimate |
| Animal Model | |
| Administration Route | |
| Output Type | in vitro functional antisense (receptor binding + protein downregulation) |
| Output Value | Decreased 125I-galanin binding to Bowes cell membranes; EC50 ~0.20 µM for h(18–38) conjugate (Table 1). Immunoprecipitation shows reduced GalR1 protein vs scrambled control. |
| Output Units | |
| Output Notes | Cells incubated with constructs at 37°C (typically 36 h for binding assays; 24 h for metabolic labeling/IP). Confocal shows internalization and broad cytosolic distribution with some nuclear accumulation; transportan localizes mainly to membranous structures. PNA sequence: GCCGTGCCCTCGCTGAGTTCCC (target human GalR1 mRNA). |
| Toxicity Notes | |
| Curation Notes |