Peptide name : 9S1R

Source/Organism : Not found

Linear/Cyclic : Linear

Chirality : L

Peptide length: 10

C-terminal modification: Linear

N-terminal modification : Free

Non-natural peptide information: None

Assay type : MTT/MTS assay

Assay time : 24h

Activity : IC50 : 9 µM

Cell line : LNCaP

Cancer type : Prostate cancer

Other activity : Not found

Amino acid composition bar chart :

Molecular mass : 1519.8051 Dalton

Aliphatic index : 0

Instability index : 317.63

Hydrophobicity (GRAVY) : -2.34

Isoelectric point : 12

Charge (pH 7) : 4.7502

Aromaticity : 0.2

Molar extinction coefficient (cysteine, cystine): (11000, 11000)

Hydrophobic/hydrophilic ratio : 0.66666666

hydrophobic moment : -0.367

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

Most occurring amino acid : R

Most occurring amino acid frequency : 5

Least occurring amino acid : C

Least occurring amino acid frequency : 1

Secondary structure fraction (Helix, Turn, Sheet): (0.1, 0.1, 0.2)

SMILES Notation: CSCC[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O

1 : Alileche A, et al. Nullomer derived anticancer peptides (NulloPs): differential lethal effects on normal and cancer cells in vitro. Peptides. 2012; 38:302-11. doi: 10.1016/j.peptides.2012.09.015

Paper title : Nullomer derived anticancer peptides (NulloPs): differential lethal effects on normal and cancer cells in vitro.

Doi : https://doi.org/10.1016/j.peptides.2012.09.015

Abstract : We demonstrate the first use of the nullomer (absent sequences) approach to drug discovery and development. Nullomers are the shortest absent sequences determined in a species, or group of species. By identifying the shortest absent peptide sequences from the NCBI databases, we screened several potential anti-cancer peptides. In order to improve cell penetration and solubility we added short poly arginine tails (5Rs), and initially solubilized the peptides in 1M trehalose. The results for one of the absent sequences 9R (RRRRRNWMWC), and its scrambled version 9S1R (RRRRRWCMNW) are reported here. We refer to these peptides derived from nullomers as PolyArgNulloPs. A control PolyArgNulloP, 124R (RRRRRWFMHW), was also included. The lethal effects of 9R and 9S1R are mediated by mitochondrial impairment as demonstrated by increased ROS production, ATP depletion, cell growth inhibition, and ultimately cell death. These effects increase over time for cancer cells with a concomitant drop in IC-50 for breast and prostate cancer cells. This is in sharp contrast to the effects in normal cells, which show a decreased sensitivity to the NulloPs over time.