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Data · dataset · 2026

Identifying protease drug targets to combat ESKAPE pathogen infections

Listed in ZivaHub and Deakin Research Online and DMU Figshare — shown once because both records carry DOI 10.17034/32805791.v1

The rise of multidrug-resistant ESKAPE pathogens has created an urgent need for novel antimicrobial strategies.

Description

Bacterial proteases, although not always essential for growth, regulate virulence, stress responses, and biofilm formation, making them attractive anti-virulence drug targets. The aim of this thesis was to investigate the roles of LonA protease, the Clp proteolytic system (ClpA and ClpS), and C13 legumain-like peptidases in Acinetobacter baumannii (A. baumannii) and Pseudomonas aeruginosa (P. aeruginosa) to evaluate their roles in virulence, biofilm formation, stress response, and their potential as anti-virulence drug targets.<br><br>In the first experimental chapter, the C13 protease of P. aeruginosa (C13-PA) was cloned and expressed in E. coli.

Unlike the homologous enzyme in A. baumannii (C13-AB), which was confirmed to be active, C13-PA showed no detectable protease activity, suggesting divergence in substrate specificity, regulation, or function.<br><br>The second chapter assessed A. baumannii transposon mutants lacking LonA, ClpA, ClpS, or C13-AB. Growth was unaffected; however, LonA and ClpA mutants displayed significantly reduced biofilm formation and attenuated virulence in the Galleria mellonella model, confirming LonA and the Clp proteostasis system as important contributors to pathogenicity.<br>The third chapter focused on LonA as a drug target.

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Minimum inhibitory concentration (MIC) and minimum biofilm eradication concentration (MBEC) assays using tigecycline showed unchanged MICs but reduced MBECs in the LonA mutant, linking LonA to biofilm antibiotic tolerance. A LonA-specific inhibitor further impaired biofilm formation and virulence, and in combination with tigecycline, produced an additive effect in biofilm reduction compared with antibiotic alone. Recombinant LonA was successfully cloned, expressed, purified, and shown to be enzymatically active against synthetic substrates, providing proof of concept for future inhibitor screening.<br><br>Overall, this work identifies LonA and the Clp proteostasis system (ClpA and ClpS) as key contributors to virulence in A. baumannii, demonstrates LonA’s role in biofilm-associated antibiotic tolerance, and highlights the potential of protease targeting as an anti-virulence strategy to enhance therapies against multidrug-resistant pathogens.<br><br><i>Thesis is embarghoed until 31 July 2029.</i><br>

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ZivaHuboai:figshare.com:article/3280579113 d agoJSON v1
Deakin Research Onlineoai:figshare.com:article/3280579113 d agoJSON v1
DMU Figshareoai:figshare.com:article/3280579113 d agoJSON v1
FieldAssertionExtractorEvidence
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concepts[field].local:field:earth-environmentalmapping · zivahub uct ac zaconnector:zivahub_uct_ac_za@1.0.0
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