dbacp06221
General Description
Peptide name : TAT-RasGAP317-326
Source/Organism : Artificial, designed
Linear/Cyclic : Not found
Chirality : Not found
Sequence Information
Sequence : RRRQRRKKRGGGDTRLNTVWMW
Peptide length: 22
C-terminal modification: Not found
N-terminal modification : Free
Non-natural peptide information: None
Activity Information
Assay type : Not specified
Assay time : Not found
Activity : Not found
Cell line : Not found
Cancer type : Not found
Other activity : Anti-microbial activity
Physicochemical Properties
Amino acid composition bar chart :
Molecular mass : 2814.2451 Dalton
Aliphatic index : 0.309
Instability index : 118.659
Hydrophobicity (GRAVY) : -2.013
Isoelectric point : 12
Charge (pH 7) : 7.7592
Aromaticity : 0.090
Molar extinction coefficient (cysteine, cystine): (11000, 11000)
Hydrophobic/hydrophilic ratio : 0.57142857
hydrophobic moment : 0.1131
Missing amino acid : C,H,P,I,E,F,S,Y,A
Most occurring amino acid : R
Most occurring amino acid frequency : 7
Least occurring amino acid : Q
Least occurring amino acid frequency : 1
Structural Information
3D structure :
Secondary structure fraction (Helix, Turn, Sheet): (0.1, 0.2, 0.2)
SMILES Notation: CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)CNC(=O)CNC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CCCNC(=N)N)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O
Secondary Structure :
| Method | Prediction |
|---|---|
| GOR | HHHHHTTTTTTCCEEEEEEEEE |
| Chou-Fasman (CF) | HHHHHHHCCCCCCEEEEEECCC |
| Neural Network (NN) | HHHHCCCCCCCCCCCHHHHEEE |
| Joint/Consensus | HHHHHCCCCCCCCEEEEEEEEE |
Molecular Descriptors and ADMET Properties
Molecular Descriptors: Click here to download
ADMET Properties: Click here to download
Cross Referencing databases
CancerPPD : Not available
ApIAPDB : Not available
CancerPPD2 ID : Not available
Reference
1 : Heulot M, et al. The Anticancer Peptide TAT-RasGAP<sub>317-326</sub> Exerts Broad Antimicrobial Activity. Front Microbiol. 2017; 8:994. doi: 10.3389/fmicb.2017.00994
Literature
Paper title : The Anticancer Peptide TAT-RasGAP<sub>317-326</sub> Exerts Broad Antimicrobial Activity.
Doi : https://doi.org/10.3389/fmicb.2017.00994
Abstract : Antibiotic resistance has become a major health issue. Nosocomial infections and the prevalence of resistant pathogenic bacterial strains are rising steadily. Therefore, there is an urgent need to develop new classes of antibiotics effective on multi-resistant nosocomial pathogenic bacteria. We have previously shown that a cell-permeable peptide derived from the p120 Ras GTPase-activating protein (RasGAP), called TAT-RasGAP<sub>317-326</sub>, induces cancer cell death, inhibits metastatic progression, and sensitizes tumor cells to various anti-cancer treatments in vitro and in vivo. We here report that TAT-RasGAP<sub>317-326</sub> also possesses antimicrobial activity. In vitro, TAT-RasGAP<sub>317-326</sub>, but not mutated or truncated forms of the peptide, efficiently killed a series of bacteria including Escherichia coli, Acinetobacter baumannii, Staphylococcus aureus, and Pseudomonas aeruginosa. In vivo experiments revealed that TAT-RasGAP<sub>317-326</sub> protects mice from lethal E. coli-induced peritonitis if administrated locally at the onset of infection. However, the protective effect was lost when treatment was delayed, likely due to rapid clearance and inadequate biodistribution of the peptide. Peptide modifications might overcome these shortcomings to increase the in vivo efficacy of the compound in the context of the currently limited antimicrobial options.