Popis: |
Publisher Summary The bacterial fatty acid biosynthesis pathway has recently generated much interest for the development of novel classes of antibacterial agents. The organization of the bacterial fatty acid synthase type II system (FASII system) based on individual enzymes is fundamentally different from the multifunctional fatty acid synthase type I system found in eukaryotes, therefore, providing good prospects for selective inhibition. All the representative targets of the FASII system have already been characterized by X-ray crystallography or nuclear magnetic resonance (NMR), which should facilitate the rational design of inhibitors. A few FASII enzymes have already been successfully validated as antibacterial targets. FASII targeting represents, therefore, an important emerging research area to address resistance issues as well as the ongoing paucity of antibacterial agents with a novel mode of action. Significant work is continued by both the academic groups and the pharmaceutical industry to validate the FASII targets and to discover relevant inhibitors. A selection of some efforts to inhibit bacterial fatty acid biosynthesis at various stages is presented in the chapter. |