Novel small molecules that increase the susceptibility of Neisseria gonorrhoeae to cationic antimicrobial peptides by inhibiting lipid A phosphoethanolamine transferase

Neisseria gonorrhoeae is an exclusively human pathogen that commonly infects the urogenital tract resulting in gonorrhoea. Empirical treatment of gonorrhoea with antibiotics has led to multidrug resistance and the need for new therapeutics. Inactivation of lipooligosaccharide phosphoethanolamine transferase A (EptA), which attaches phosphoethanolamine to lipid A, results in attenuation of the pathogen in infection models.

Citation:
Mullally C, Stubbs KA, Thai VC, Anandan A, ……… Kahler CM. Novel small molecules that increase the susceptibility of Neisseria gonorrhoeae to cationic antimicrobial peptides by inhibiting lipid A phosphoethanolamine transferase. J Antimicrob Chemother. 2022;77(9):2441-7.

Keywords:
Anti-infective agent; antimicrobial cationic peptide; ethanolamine derivative;
ethanolamine phosphotransferase; lipid A; phosphoethanolamine; antibiotic resistance; gonorrhea; microbial sensitivity test; Neisseria; Anti-Bacterial Agents; Drug Resistance

Abstract:
Neisseria gonorrhoeae is an exclusively human pathogen that commonly infects the urogenital tract resulting in gonorrhoea. Empirical treatment of gonorrhoea with antibiotics has led to multidrug resistance and the need for new therapeutics. Inactivation of lipooligosaccharide phosphoethanolamine transferase A (EptA), which attaches phosphoethanolamine to lipid A, results in attenuation of the pathogen in infection models.