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Researchers from the University of Eastern Finland have identified new compounds that can target bacterial infection and provide a potential response to antibiotic resistance.
Image credit: Kateryna Kon / Shutterstock
As reported in the journal ChemMedChem Prasanthi Medarametla and colleagues targeted a protein called LsrK which is involved in a process of bacterial communication called quorum sensing.
Quorum sensing allows bacteria to colonize, produce virulence factors, form a biofilm and establish infection.
Disturbance The quorum detection process has therefore become a new center of interest in the search for agents likely to smother and inhibit bacteria.
At the time of With increased antibiotic resistance, targeting the enzymes involved in bacterial communication (quorum sensing) is a new strategy for fighting bacterial infections. "
Prasanthi Medarame tla, principal investigator
The detection of quorum is induced by molecules called self-inducing (IA) and a signaling molecule called AI -2 is essential for intraspecific and interspecific bacterial communication
Phosphorylation of AI-2 is mediated by the LsrK enzyme, which means that the inhibition of this protein can inactivate the detection of quorum. However, to date, no LsrK inhibitor of this type has been reported.
Medarametla and his colleagues have now used computational methods to model the structure of LsrK and screened a library of compounds to find potential inhibitors of the protein.
the team identified four results of micromolar activity against LsrK.
The LsrK inhibitors identified by the team will be further developed to ensure high affinity and function, so that they can be used as tools to help researchers understand how to inhibit LsrK in l & # 39; AI.
Given the limited knowledge we have about the structure of LsrK, this study provides interesting new information about the behavior of the protein and how to potentially interfere with the protein-substrate dynamics that provide virulence. .
prove the utility of the model and provide the first clbad of LsrK inhibitors with additional optimization as antivirulent agents. "
Prasanthi Medarametla, Principal Investigator [19659] 017] Sources:
New Antibacterial Drugs Developed at the University of Eastern Finland.
Virtual Screening Based on Inhibitor Structure of LsrK kinase to target quorum detection
