Click-Free Synthesis of a Multivalent Tricyclic Peptide as a Molecular Transporter (2020)
Tricyclic peptide 20 ([(WR)4]3)
Sequence: Tricyclic polycyclic peptide, trimer of cyclic (WRWRWRWR) units linked via amide bonds (reported as [(WR)4]3)
| Experiment Id | EXP001620 |
|---|---|
| Paper | Click-Free Synthesis of a Multivalent Tricyclic Peptide as a Molecular Transporter |
| Peptide | Tricyclic peptide 20 ([(WR)4]3) |
| Delivery Success Class | no |
| In Vivo Flag | no |
| Uptake Confirmed | yes |
| Label Confidence | high |
| In Vitro Functional Effect | no |
| Endosomal Escape Evidence | |
| Peptide Concentration | Complexed with siRNA at N/P ratios 10, 20, 40 (peptide stock 1 mM; final molarity not explicitly stated) |
| Rna Concentration | Not explicitly stated (FAM-siRNA in 150 mM NaCl; amount not specified) |
| Mixing Ratio | N/P = 10, 20, 40 (peptide:siRNA) |
| Formulation Format | Electrostatic peptide/siRNA complexes (simple mixing; 30 min incubation) |
| Formulation Components | Tricyclic peptide 20 + FAM-siRNA in 150 mM NaCl (no additional excipients reported) |
| Size Nm | |
| Zeta Mv | |
| Model Scope | in_vitro |
| Model Type | in vitro |
| Cell Lines Or Primary Cells | MDA-MB-231 (human breast cancer) cells |
| Animal Model | |
| Administration Route | |
| Output Type | uptake (flow cytometry) |
| Output Value | ~3.3-fold increase in siRNA internalization vs siRNA alone at N/P 10; reduced effect at N/P 20 and ~no difference at N/P 40 |
| Output Units | |
| Output Notes | Uptake quantified by flow cytometry after 24 h incubation; complexes formed by mixing and standing 30 min |
| Toxicity Notes | >97% cell viability up to 25 µM; ~92% at 30 µM (MTS assay, 24 h) |
| Curation Notes |