Abstract
Methicillin-resistant (MRSA) causing serious hospital-acquired infections and skin infections has become a "superbug" in clinical treatment. Although the clinical treatment of MRSA is continuously improving, due to its unceasing global spread, MRSA has produced much heated discussion and focused study, therefore suggesting an urgent task to find new antibacterial drugs to combat this issue. Antimicrobial peptides (AMPs) are used as the last-resort drugs for treating multidrug-resistant bacterial infections, but their utilisation is still limited due to their low stability and often strong toxicity. Here, we evaluated the structure and the bioactivity of an AMP, GV30, derived from the frog skin secretions of and designed seven truncated derivatives based on the presence of cleavage sites for trypsin using an online proteomic bioinformatic resource PeptideCutter tool. We investigated the anti-MRSA effect, toxicity and salt- and serum-resistance of these peptides. Interestingly, the structure-activity relationship revealed that removing "Rana box" loop could significantly improve the bactericidal speed on MRSA. Among these derivatives, GV21 (GVIFNALKGVAKTVAAQLLKK-NH ), because of its faster antibacterial effect, lower toxicity, and retains the good antibacterial activity and stability of the parent peptide, is considered to become a new potential antibacterial candidate against MRSA.
Original language | English |
---|---|
Pages (from-to) | 4984-4996 |
Journal | Computational and Structural Biotechnology Journal |
Volume | 19 |
Early online date | 29 Aug 2021 |
DOIs | |
Publication status | Early online date - 29 Aug 2021 |
Keywords
- Antibacterial effect
- Antimicrobial peptides
- Methicillin-resistant Staphylococcus aureus
- PeptideCutter tool
- Salt- and serum-resistance
- Toxicity
- Truncated derivatives
Fingerprint
Dive into the research topics of 'Generation of truncated derivatives through in silico enzymatic digest of peptide GV30 target MRSA both in vitro and in vivo'. Together they form a unique fingerprint.Student theses
-
Functional optimisation and structure-activity relationship studies of helix-loop peptides from the skin secretions of the frogs, Odorrana schmackeri and Amolops wuyiensis
Yao, A. (Author), Zhou, M. (Supervisor) & Wang, L. (Supervisor), Jul 2022Student thesis: Doctoral Thesis › Doctor of Philosophy
-
Rational design and engineering of antimicrobial peptides found from natural sources
Ma, Y. (Author), Zhou, M. (Supervisor) & Wang, L. (Supervisor), Jul 2022Student thesis: Doctoral Thesis › Doctor of Philosophy