Design, Synthesis, and Evaluation of New 1H-Benzo[d]imidazole Based PqsR Inhibitors as Adjuvant Therapy for Pseudomonas aeruginosa Infections

Soukarieh, Fadi; Mashabi, Alaa; Richardson, William; Oton, Eduard Vico; Romero, Manuel; Dubern, Jean-Frédéric; Robertson, Shaun N.; Lucanto, Simone; Markham-Lee, Zoe; Sou, Tomás; Kukavica-Ibrulj, Irena; Levesque, Roger C.; Bergstrom, Christel A.S.; Halliday, Nigel; Kellam, Barrie; Emsley, Jonas; Heeb, Stephan; Williams, Paul; Stocks, Michael J.; Cámara, Miguel

doi:10.1021/acs.jmedchem.3c00973

All Outputs (3)

CXCL17 is an allosteric inhibitor of CXCR4 through a mechanism of action involving glycosaminoglycans (2024)
Journal Article

CXCL17 is a chemokine principally expressed by mucosal tissues, where it facilitates chemotaxis of monocytes, dendritic cells, and macrophages and has antimicrobial properties. CXCL17 is also implicated in the pathology of inflammatory disorders and... Read More about CXCL17 is an allosteric inhibitor of CXCR4 through a mechanism of action involving glycosaminoglycans.

A time-resolved Förster resonance energy transfer assay to investigate drug and inhibitor binding to ABCG2 (2024)
Journal Article

The human ATP-binding cassette (ABC) transporter, ABCG2, is responsible for multidrug resistance in some tumours. Detailed knowledge of its activity is crucial for understanding drug transport and resistance in cancer, and has implications for wider... Read More about A time-resolved Förster resonance energy transfer assay to investigate drug and inhibitor binding to ABCG2.

Design, Synthesis, and Evaluation of New 1H-Benzo[d]imidazole Based PqsR Inhibitors as Adjuvant Therapy for Pseudomonas aeruginosa Infections (2024)
Journal Article

Pseudomonas aeruginosa is one of the top priority pathogens that requires immediate attention according to the World Health Organisation (WHO). Due to the alarming shortage of novel antimicrobials, targeting quorum sensing (QS), a bacterial cell to c... Read More about Design, Synthesis, and Evaluation of New 1H-Benzo[d]imidazole Based PqsR Inhibitors as Adjuvant Therapy for Pseudomonas aeruginosa Infections.