webinar recording: a strategy to combat multidrug-resistant bacteria

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Approved drugs containing thiols as inhibitors of Metallo-β-Lactamases

Antibiotic resistance in bacterial pathogens is one of the major threats regarding human health. An alarming trend is the spread of metallo-β-lactamases (MBLs) among gram-negative pathogens that transfer resistance against almost all β-lactam antibiotics including carbapenems. The development of new anti-infective agents remains one of the most significant demands in modern medicine.

In this webinar we show the development of an assay platform consisting of three orthogonal assays: a fluorescence-based functional assay, thermal shift assay and in cell antimicrobial susceptibility testing. The reliability of the system was evaluated on three different class B MBLs: New-Delhi-Metallo-β-Lactamase-1 (NDM-1), Verona-Integron-Encoded-Metallo-β-Lactamase 1 (VIM-1) and Impenemase-7 (IMP-7).

The aim of this work is to find an already approved drug which restores the activity of β-lactam antibiotic by protecting it from hydrolysis through the MBL. We could find four drugs, which inhibit three clinically important MBLs, namely Captopril, Thiorphan, Dimercaprol and Tiopronin. This is a good starting point for the development of potent MBL inhibitors, with the primary optimization goal being the uptake and activity in pathogens. This will be modeled in SeeSAR.



Ashfaq Ahmad says:

Madam, Can I have you PPT at my inbox. ashfaqahmad82@hotmail.com

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