Peptide name : PTP4

Source/Organism : Skin of a Korean frog, Wrinkled frog

Linear/Cyclic : Linear

Chirality : L

Peptide length: 24

C-terminal modification: Linear

N-terminal modification : Free

Non-natural peptide information: None

Assay type : MTT/MTS assay

Assay time : 96h

Activity : IC50 : 26.15 µg/ml

Cell line : HEK296

Cancer type : Renal cancer

Other activity : Not found

Amino acid composition bar chart :

Molecular mass : 2783.5687 Dalton

Aliphatic index : 1.383

Instability index : -0.0792

Hydrophobicity (GRAVY) : 0.7875

Isoelectric point : 9.929

Charge (pH 7) : 5.7333

Aromaticity : 0.125

Molar extinction coefficient (cysteine, cystine): (1490, 1615)

Hydrophobic/hydrophilic ratio : 1.66666666

hydrophobic moment : 0.2702

Missing amino acid : R,W,H,Q,M,E,D,N,V,G

Most occurring amino acid : K

Most occurring amino acid frequency : 6

Least occurring amino acid : P

Least occurring amino acid frequency : 1

Secondary structure fraction (Helix, Turn, Sheet): (0.5, 0.0, 0.5)

SMILES Notation: CC[C@H](C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(=O)O

1 : Kim S, et al. In vitro activities of native and designed peptide antibiotics against drug sensitive and resistant tumor cell lines. Peptides. 2003; 24:945-53. doi: 10.1016/s0196-9781(03)00194-3

Paper title : In vitro activities of native and designed peptide antibiotics against drug sensitive and resistant tumor cell lines.

Doi : https://doi.org/10.1016/s0196-9781(03)00194-3

Abstract : In order to develop peptide agents with reduced length and enhanced tumoricidal activity, we have designed gaegurin 6 (GGN6) derivatives through deletions and/or substitutions of amino acids. The deletion of hydrophobic amino terminal region completely abolished antitumor activity whereas the deletion of carboxy terminal region had little influence on antitumor activity. Antitumor activity of the PTP peptides did not correlate with antibacterial activity. PTP7, the most potent derivative, was found to have comparable antitumor activity to GGN6 in spite of reduced number of amino acids which is about half the size of gaegurin 6; furthermore, it showed little cytotoxicity on PBMCs and RBCs. GGN6 and PTP7 also showed equivalent cytotoxicity against drug sensitive (MCF-7) and multidrug-resistant cell lines (MCF-7/DOX). Plasma membrane blebbing and DNA fragmentation of peptide-treated tumor cells indicated that the peptides could induce apoptosis in tumor cells. These results suggest that GGN6 and its derivatives can be developed as new anticancer agents and may provide a new strategy for overcoming MDR which is a major problem in cancer therapy.