LpxC
Gram-negative bacteria differ from Gram-positive bacteria in that they possess a unique outer membrane, with the outer leaflet of the outer membrane enriched with lipid A, the membrane anchor of lipopolysaccharide (LPS) and the active component of bacterial endotoxin[1]. LpxC (UDP-3-O-(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase; EC 3.5.1.108) is a metalloenzyme that catalyzes the first committed step in the biosynthesis of lipid A, an essential component of the outer membrane of Gram-negative bacteria. As such, LpxC is an attractive antibacterial target as there is no human homologue and it is highly conserved in Gram-negative bacteria. The LpxC inhibitors block LPS synthesis by blockade of the sepsis cascade, and show enhanced opsonophagocytic killing of the bacteria[2].
[1] X. Liang et al. Synthesis, Structure, and Antibiotic Activity of Aryl-Substituted LpxC Inhibitors. J. Med. Chem., 2013, 56, 6954-6966.
[2] Pyridone Methylsulfone Hydroxamate LpxC Inhibitors for the Treatment of Serious Gram-Negative Infections. Justin I. Montgomery et al. J. Med. Chem., 2012, 55, 1662-1670.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 2000 | CHIR090 | Potent and selective LpxC inhibitor | €135.00 | |
| 2113 | PF 05081090 | LpxC inhibitor for treatment of gram-negative infections | €160.00 | |
| 1939 | PF-04753299 | Potent antibacterial LpxC inhibitor (gram-negative infections) | €95.00 | |