Peptide name : Dual-functional peptide LPLTPLP

Source/Organism : Not found

Linear/Cyclic : Linear

Chirality : L

Peptide length: 7

C-terminal modification: Linear

N-terminal modification : Not found

Non-natural peptide information: None

Assay type : CCK-8 assay

Assay time : 24h

Activity : IC50 : 0.00022 M

Cell line : A549

Cancer type : Lung cancer

Other activity : Not found

Amino acid composition bar chart :

Molecular mass : 749.9376 Dalton

Aliphatic index : 1.671

Instability index : 63.6

Hydrophobicity (GRAVY) : 0.8429

Isoelectric point : 5.525

Charge (pH 7) : -0.2399

Aromaticity : 0

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

Hydrophobic/hydrophilic ratio : 6

hydrophobic moment : -0.454

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

Most occurring amino acid : L

Most occurring amino acid frequency : 3

Least occurring amino acid : T

Least occurring amino acid frequency : 1

Secondary structure fraction (Helix, Turn, Sheet): (0.4, 0.4, 0.5)

SMILES Notation: CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CC(C)C)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N1CCC[C@H]1C(=O)O)[C@@H](C)O

1 : Jiang Y, et al. Enhanced in vivo antitumor efficacy of dual-functional peptide-modified docetaxel nanoparticles through tumor targeting and Hsp90 inhibition. J Control Release. 2016; 221:26-36. doi: 10.1016/j.jconrel.2015.11.029

Paper title : Enhanced in vivo antitumor efficacy of dual-functional peptide-modified docetaxel nanoparticles through tumor targeting and Hsp90 inhibition.

Doi : https://doi.org/10.1016/j.jconrel.2015.11.029

Abstract : Although conventional anticancer drugs exhibit excellent efficacy, serious adverse effects and/or even toxicity have occurred due to their nonselectivity. Moreover, active targeting approaches have not consistently led to successful outcomes. Ligands that simultaneously possess targeting capability and exert a strong influence on intracellular signaling cascades may be expected to improve the therapeutic efficacy of active targeting nanoparticulate carriers. In this study, we screened a targeting peptide, LPLTPLP, which specifically bound to non-small cell lung cancer (NSCLC) specimens in vitro. Surprisingly, this peptide inhibited the expression of Hsp90 and induced apoptosis by preventing autophagy in A549 cells treated with docetaxel. The results suggested that this peptide might be used as a promising dual-functional ligand for cancer treatment. Based on these findings, we designed and developed a novel active targeting delivery system by modifying docetaxel nanoparticles (DNP) with the dual-functional ligand LPLTPLP. We consistently demonstrated that the cellular uptake of nanoparticles (NPs) was significantly enhanced in vitro. Furthermore, the targeting NPs exhibited significantly improved antitumor efficacy and biodistribution compared with nontargeting nanodrug and free docetaxel. These findings demonstrate the feasibility of dual-functional NPs for efficient anticancer therapy.