Peptide name : Pep-1-Phor21

Source/Organism : Hybrid peptide PEP1 and Phor 21

Linear/Cyclic : Linear

Chirality : L

Peptide length: 30

C-terminal modification: Linear

N-terminal modification : Free

Non-natural peptide information:

Assay type : AlamarBlue assay

Assay time : 24-h

Activity : IC50 = 2.57 ± 2.02 µM

Cell line : DU-145

Cancer type : Prostrate Cancer

Other activity : Anticancer

Amino acid composition bar chart :

Molecular mass : 3503.3012 Dalton

Aliphatic index : 0.296

Instability index : 8.4367

Hydrophobicity (GRAVY) : -0.203

Isoelectric point : 10.317

Charge (pH 7) : 8.7341

Aromaticity : 23.33

Molar extinction coefficient (cysteine, cystine): (2, 1)

Hydrophobic/hydrophilic ratio : 1.7273

hydrophobic moment : 0.1332

Missing amino acid : D,H,I,L,N,P,Q,S,T,Y

Most occurring amino acid : K

Most occurring amino acid frequency : 9

Least occurring amino acid : E

Least occurring amino acid frequency : 1

Secondary structure fraction (Helix, Turn, Sheet): (56., 6.6, 26.)

SMILES Notation: CSCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H](N)CS)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)O)C(C)C

1 : Jannoo R, et al. Targeting of the Interleukin-13 Receptor (IL-13R)α2 Expressing Prostate Cancer by a Novel Hybrid Lytic Peptide. Biomolecules. 2023; 13:(unknown pages). doi: 10.3390/biom13020356

Paper title : Targeting of the Interleukin-13 Receptor (IL-13R)α2 Expressing Prostate Cancer by a Novel Hybrid Lytic Peptide.

Doi : https://doi.org/10.3390/biom13020356

Abstract : The IL-13Rα2 cell surface receptor is highly expressed in tumours such as prostate cancer. In this report, we evaluated the hypothesis that prostate cancer cells with enhanced IL-13Rα2 expression are a suitable target for the hybrid lytic peptide (Pep-1-Phor21) peptide, which is generated by fusing the IL-13Rα2 specific ligand (Pep-1) and a cell membrane disrupting lytic peptide (Phor21). The expression of IL-13Rα2 mRNA and protein in prostate cancer tissues and cell lines was assessed via real-time PCR (RT-PCR) and immunoblotting. The effect of Pep-1-Phor21 on the viability of prostate cancer cells grown in monolayers (2D) and microtissue spheroids (3D) was assessed via CellTox green cytotoxic assay. IL-13Rα2 expression and Pep-1-Phor21-mediated killing were also determined in the cells treated with epigenetic regulators (Trichostatin A (TSA) and 5-aza-2 deoxycytidine (5-Aza-dC)). The hybrid lytic peptide cytotoxic activity correlated with the expression of IL-13Rα2 in prostate cancer cell lines cultured as monolayers (2D) or 3D spheroids. In addition, TSA or 5-Aza-dC treatment of prostate cancer cells, particularly those with low expression of IL-13Rα2, enhanced the cells' sensitivity to the lytic peptide by increasing IL-13Rα2 expression. These results demonstrate that the Pep-1-Phor21 hybrid lytic peptide has potent and selective anticancer properties against IL-13Rα2-expressing prostate cancer cells.