NGR motif peptide + CPP (penetratin-derived)
Sequence: CYGGRGNG ; CKRRMKWKK
| Experiment Id | EXP000515 |
|---|---|
| Paper | Dual stimulus of hyperthermia and intracellular redox environment triggered release of siRNA for tum |
| Peptide | NGR motif peptide + CPP (penetratin-derived) |
| Delivery Success Class | no |
| In Vivo Flag | no |
| Uptake Confirmed | yes |
| Label Confidence | high |
| In Vitro Functional Effect | yes |
| Endosomal Escape Evidence | yes |
| Peptide Concentration | |
| Rna Concentration | 250 nM (gene knockdown assays); 100 nM (uptake assays) |
| Mixing Ratio | |
| Formulation Format | Thermosensitive liposome (TSL) with NGR targeting; encapsulated siRNA-CPP conjugate; heat-triggered release |
| Formulation Components | DPPC:MSPC:DSPE-PEG2000-NGR (87:3:10, w/w); encapsulated siRNA-CPP conjugate; hyperthermia 42°C 30 min to trigger release/activate CPP; intracellular GSH reduces disulfide |
| Size Nm | 90.23 |
| Zeta Mv | -18.98 |
| Model Scope | in_vitro |
| Model Type | in vitro |
| Cell Lines Or Primary Cells | HT-1080 (human fibrosarcoma, CD13 high) |
| Animal Model | |
| Administration Route | |
| Output Type | Gene knockdown (qRT-PCR / western blot); uptake (FACS/CLSM); endosomal escape (LysoTracker colocalization) |
| Output Value | Significant c-myc mRNA/protein inhibition for heat-activated NGR-TSL formulation |
| Output Units | |
| Output Notes | Formulation referred to as siRNA-CPPs/NGR-TSL-H (preheated 42°C, 30 min). Unheated NGR-TSL largely endosomally trapped and showed only slight knockdown. |
| Toxicity Notes | In vitro apoptosis increased with heat-activated NGR-TSL vs controls |
| Curation Notes |