Katrin Voos

Inhibitors of the Elastase LasB for the Treatment of Pseudomonas aeruginosa Lung Infections

Jelena Konstantinović, Andreas M. Kany, Alaa Alhayek, Ahmed Saad Abdelsamie et autres

High Resolution Image Download MS PowerPoint Slide Infections caused by the Gram-negative pathogen Pseudomonas aeruginosa are emerging worldwide as a major threat to human health. Conventional antibiotic monotherapy suffers from rapid resistance development, underlining urgent need for novel treatment concepts. Here, we …

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Inhibitors of the Elastase LasB for the treatment of Pseudomonas aeruginosa lung infections

Jelena Konstantinović, Andreas M. Kany, Alaa Alhayek, Ahmed Saad Abdelsamie et autres

Infections caused by the Gram-negative pathogen Pseudomonas aeruginosa are emerging worldwide as a major threat to human health. Conventional antibiotic monotherapy suffers from rapid resistance development, underlining urgent need for novel treatment concepts. Here, we report on a non-traditional approach to combat …

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N-Aryl-2-iso-butylmercaptoacetamides: the discovery of highly potent and selective inhibitors of Pseudomonas aeruginosa virulence factor LasB and Clostridium histolyticum virulence factor ColH

Katrin Voos, Samir Yahiaoui, Jelena Konstantinović, Esther Schönauer et autres

Antimicrobial resistance is currently one of the serious global public health threats. Unlike the conventional antimicrobial drugs, antivirulence agents disarm rather than kill bacterial pathogens and therefore represent an alternative option to skirt the problem of resistance. Pseudomonas aeruginosa elastase (LasB) and …

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Inhibition of Collagenase Q1 of Bacillus cereus as a Novel Antivirulence Strategy for the Treatment of Skin‐Wound Infections

Alaa Alhayek, Essak S. Khan, Esther Schönauer, Tobias Däinghaus et autres

Abstract Despite the progress in surgical techniques and antibiotic prophylaxis, opportunistic wound infections with Bacillus cereus remain a public health problem. Secreted toxins are one of the main factors contributing to B. cereus pathogenicity. A promising strategy to treat such infections is …

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Inhibition of Collagenase Q1 of Bacillus cereus as a Novel Antivirulence Strategy for the Treatment of Skin-Wound Infections

Alaa Alhayek, Essak S. Khan, Esther Schönauer, Tobias Däinghaus et autres

Despite the progress in surgical techniques and antibiotic prophylaxis, opportunistic wound infections with Bacillus cereus remain a public health problem. Secreted toxins are one of the main factors contributing to B. cereus pathogenicity. A promising strategy to treat such infections is to …

Front Cover: Phosphonate as a Stable Zinc‐Binding Group for “Pathoblocker” Inhibitors of Clostridial Collagenase H (ColH) (ChemMedChem 8/2021)

Katrin Voos, Esther Schönauer, Alaa Alhayek, Jörg Haupenthal et autres

The Front Cover shows work on inhibitors of bacterial collagenases. The inhibition of these virulence factors would reduce bacterial pathogenicity, thus furnishing a potential “pathoblocker”. Previously reported inhibitors of zinc-dependent collagenases employed a thiol function as zinc-binding group (ZBG). The researchers have …

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Phosphonate as a Stable Zinc‐Binding Group for “Pathoblocker” Inhibitors of Clostridial Collagenase H (ColH)

Katrin Voos, Esther Schönauer, Alaa Alhayek, Jörg Haupenthal et autres

Microbial infections are a significant threat to public health, and resistance is on the rise, so new antibiotics with novel modes of action are urgently needed. The extracellular zinc metalloprotease collagenase H (ColH) from Clostridium histolyticum is a virulence factor that catalyses …

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N -Aryl mercaptoacetamides as potential multi-target inhibitors of metallo-β-lactamases (MBLs) and the virulence factor LasB from Pseudomonas aeruginosa

Samir Yahiaoui, Katrin Voos, Jörg Haupenthal, Thomas A. Wichelhaus et autres

isolates, where they restored the full activity of imipenem. Together with their LasB-inhibitory activity in the micromolar range, this class of compounds can now serve as a starting point for a multi-target inhibitor approach against both bacterial resistance and virulence, which is …

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Discovery of a Potent Inhibitor Class with High Selectivity toward Clostridial Collagenases

Esther Schönauer, Andreas M. Kany, Jörg Haupenthal, Kristina Hüsecken et autres

Secreted virulence factors like bacterial collagenases are conceptually attractive targets for fighting microbial infections. However, previous attempts to develop potent compounds against these metalloproteases failed to achieve selectivity against human matrix metalloproteinases (MMPs). Using a surface plasmon resonance-based screening complemented with enzyme …

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