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EXP000640

Paper

Design of cyclic RGD-conjugated Aib-containing amphipathic helical peptides for targeted delivery of small interfering RNA (2016)

Peptide

PI

Sequence: Acetyl-KLULKLULKULKAULKLUGC(cRGDfC)-NH2

RNA

siRNA

All experiment fields

Experiment Id EXP000640
Paper Design of cyclic RGD-conjugated Aib-containing amphipathic helical peptides for targeted delivery of
Peptide PI
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 1.0 µM
Rna Concentration 10 nM
Mixing Ratio 100
Formulation Format electrostatic peptide/siRNA complex
Formulation Components cRGDfC–MAP(Aib) conjugate peptide + siRNA (complex formed by electrostatic interaction)
Size Nm
Zeta Mv
Model Scope in_vitro
Model Type in vitro
Cell Lines Or Primary Cells A549; A549-Luc (luciferase-expressing A549)
Animal Model
Administration Route
Output Type reporter knockdown (luciferase)
Output Value 10.2% relative luciferase activity (vs control) at 24 h post-treatment
Output Units
Output Notes Complexation: gel retardation complete at peptide/siRNA ≥50–100. Uptake/CLSM: strong uptake in A549; uniform + punctate intracellular fluorescence; partial colocalization with LysoTracker (endosome/lysosome). RNAi: strong knockdown at 1.0 µM peptide /10 nM siRNA (ratio 100) after 8 h incubation + 24 h culture; strongest at ratio 50; ratio 20 comparable to Lipofectamine 2000.
Toxicity Notes LDH release ~20% at 1.0 µM/10 nM (ratio 100) after 24 h; reduced to ~12% (ratio 50) and ~7% (ratio 20).
Curation Notes