Peptide name : D-FP21-PEG-PEI/pGRO-α

Source/Organism : Synthetic

Linear/Cyclic : Linear

Chirality : D

Peptide length: 21

C-terminal modification: Linear

N-terminal modification : Free

Non-natural peptide information: conjugated to polyethylenimine (PEI) and methoxy polyethylene glycol (mPEG)

Assay type : CCK-8 assay

Assay time : 24-h

Activity : IC50 = 21.6 μg/mL

Cell line : HO-8910

Cancer type : Ovarian Cancer

Other activity : Anti-caner, anti-proliferative, anti-tumor

Amino acid composition bar chart :

Molecular mass : 2284.4823 Dalton

Aliphatic index : 0

Instability index : 5.8952

Hydrophobicity (GRAVY) : -0.566

Isoelectric point : 5.9597

Charge (pH 7) : -0.2397

Aromaticity : 14.28

Molar extinction coefficient (cysteine, cystine): (0, 0)

Hydrophobic/hydrophilic ratio : infinite

hydrophobic moment : 0

Missing amino acid : A,C,D,E,F,G,H,I,K,L,M,N,P,Q,R,S,T,V,W,Y

Most occurring amino acid : g

Most occurring amino acid frequency : 4

Least occurring amino acid : l

Least occurring amino acid frequency : 1

Secondary structure fraction (Helix, Turn, Sheet): (9.5, 38., 42.)

SMILES Notation: CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)O)[C@@H](C)O)[C@@H](C)O

1 : Zhang M, et al. Retro-inverso follicle-stimulating hormone peptide-mediated polyethylenimine complexes for targeted ovarian cancer gene therapy. Drug Deliv. 2018; 25:995-1003. doi: 10.1080/10717544.2018.1461956

Paper title : Retro-inverso follicle-stimulating hormone peptide-mediated polyethylenimine complexes for targeted ovarian cancer gene therapy.

Doi : https://doi.org/10.1080/10717544.2018.1461956

Abstract : BACKGROUND: The development of nanoparticle drug delivery systems with targeted ligands has the potential to increase treatment efficiency in ovarian cancer. METHODS: We developed a 21-amino acid peptide, YTRDLVYGDPARPGIQGTGTF (L-FP21) conjugated to polyethylenimine (PEI) and methoxy polyethylene glycol (mPEG) to prepare a nanoparticle drug vehicle to target follicle-stimulating hormone receptor (FSHR) in ovarian cancer. At the same time, we optimized the ligand of the nanoparticle vehicle using D-peptides, which consist of D-amino acids (D-FP21). Nanoparticle vehicles carrying the therapeutic gene plasmid growth-regulated oncogene alpha (pGRO-α) short hairpin RNA (shRNA) (FP21-PEG-PEI/pGRO-α) were prepared for further investigation. RESULTS: Compared with L-FP21, D-FP21 exhibited improved biological stability and higher uptake rate for FSHR-expressing ovarian cancer cells. The cytotoxicity of the L, D-FP21-PEG-PEI/pGRO-α complexes were significantly lower than that of the PEI/pGRO-α complex. The nanoparticle drug with the targeted ligand showed higher transfection efficiencies and improved anti-proliferation effects for ovarian cancer cells than that without the targeted ligand (mPEG-PEI/pGRO-α). Furthermore, an in vivo evaluation of an antitumor assay indicated that D-FP21-PEG-PEI/pGRO-α inhibited the growth of tumor spheroids considerably more than L-FP21-PEG-PEI/pGRO-α; their tumor inhibition rates were 58.5% and 33.3%, respectively. CONCLUSIONS: D-FP21-PEG-PEI/plasmid DNA is a safe and efficient gene delivery vehicle for ovarian cancer targeted therapy.