Sequence: cyclo(RGDfK); main text reports cyclo-RGDfK/cRGD peptide, with N-terminal cysteine used for conjugation
| Experiment Id | EXP002506 |
|---|---|
| Paper | Multifunctional polyion complex micelle featuring enhanced stability, targetability, and endosome es |
| Peptide | cRGD-PEG-PAsp(TEP)-Chol |
| Delivery Success Class | yes |
| In Vivo Flag | yes |
| Uptake Confirmed | yes |
| Label Confidence | high |
| In Vitro Functional Effect | |
| Endosomal Escape Evidence | |
| Peptide Concentration | |
| Rna Concentration | 25 µg siRNA/mouse/injection; 8 total injections for therapy; 2 injections for qRT-PCR knockdown study |
| Mixing Ratio | N/P = 3 |
| Formulation Format | targeted/stabilized polyion complex micelle |
| Formulation Components | cRGD-PEG-PAsp(TEP)-Chol block copolymer complexed with siPlk1; PEG shell, cRGD targeting ligand, PAsp(TEP) cationic/endosome-disrupting segment, cholesteryl stabilizing moiety |
| Size Nm | -50.00 |
| Zeta Mv | |
| Model Scope | in_vivo |
| Model Type | in vivo therapeutic gene silencing |
| Cell Lines Or Primary Cells | A549 human lung carcinoma xenograft |
| Animal Model | BALB/c nude mice bearing subcutaneous A549 tumors |
| Administration Route | intravenous tail vein |
| Output Type | tumor growth inhibition and target mRNA knockdown |
| Output Value | significant tumor growth inhibition and ~30% PLK1 mRNA reduction in tumor tissue compared with siScr micelle and buffer controls |
| Output Units | |
| Output Notes | Functional in vivo RNAi was sequence-specific: siPlk1 micelle reduced PLK1 mRNA and inhibited A549 tumor growth, while siScr micelle did not. |
| Toxicity Notes | Negligible liver toxicity: ALT and AST were not significantly different from control after cRGD-PEG-PAsp(TEP)-Chol/siScr micelle administration. |
| Curation Notes |