Peptide name : Peptide13 Gonearrestide

Source/Organism : Androctonus mauritanicus

Linear/Cyclic : Linear

Chirality : L

Peptide length: 18

C-terminal modification: Linear

N-terminal modification : Amidation

Non-natural peptide information:

Assay type : MTT assay

Assay time : 24-h

Activity : IC50 ~ 100 μM/L

Cell line : HCT-116

Cancer type : Colon Cancer

Other activity : Anticancer

Amino acid composition bar chart :

Molecular mass : 2195.5665 Dalton

Aliphatic index : 0.594

Instability index : -2.3833

Hydrophobicity (GRAVY) : -1.038

Isoelectric point : 9.306

Charge (pH 7) : 2.7402

Aromaticity : 11.11

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

Hydrophobic/hydrophilic ratio : 0.8

hydrophobic moment : -0.073

Missing amino acid : A,F,H,M,Q,T

Most occurring amino acid : K

Most occurring amino acid frequency : 3

Least occurring amino acid : W

Least occurring amino acid frequency : 1

Secondary structure fraction (Helix, Turn, Sheet): (27., 27., 27.)

SMILES Notation: CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(N)=O)C(=O)O

1 : Li B, et al. Triggering of cancer cell cycle arrest by a novel scorpion venom-derived peptide-Gonearrestide. J Cell Mol Med. 2018; 22:4460-4473. doi: 10.1111/jcmm.13745

Paper title : Triggering of cancer cell cycle arrest by a novel scorpion venom-derived peptide-Gonearrestide.

Doi : https://doi.org/10.1111/jcmm.13745

Abstract : In this study, a novel scorpion venom-derived peptide named Gonearrestide was identified in an in-house constructed scorpion venom library through a combination of high-throughput NGS transcriptome and MS/MS proteome platform. In total, 238 novel peptides were discovered from two scorpion species; and 22 peptides were selected for further study after a battery of functional prediction analysis. Following a series of bioinformatics analysis alongside with in vitro biological functional screenings, Gonearrestide was found to be a highly potent anticancer peptide which acts on a broad spectrum of human cancer cells while causing few if any observed cytotoxic effects on epithelial cells and erythrocytes. We further investigated the precise anticancer mechanism of Gonearrestide by focusing on its effects on the colorectal cancer cell line, HCT116. NGS RNA sequencing was employed to obtain full gene expression profiles in HCT116 cells, cultured in the presence and absence of Gonearrestide, to dissect signalling pathway differences. Taken together the in vitro, in vivo and ex vivo validation studies, it was proven that Gonearrestide could inhibit the growth of primary colon cancer cells and solid tumours by triggering cell cycle arrest in G1 phase through inhibition of cyclin-dependent kinases 4 (CDK4) and up-regulate the expression of cell cycle regulators/inhibitors-cyclin D3, p27, and p21. Furthermore, prediction of signalling pathways and potential binding sites used by Gonearrestide are also presented in this study.