School of Biomedical Sciences, Charles Sturt University, Wagga Wagga, NSW, 2678, Australia.
College of Science and Engineering, Flinders University, Bedford Park, SA, 5042, Australia.
Sci Rep. 2021 Mar 29;11(1):7050. doi: 10.1038/s41598-021-86400-1.
Treatments for 'superbug' infections are the focus for innovative research, as drug resistance threatens human health and medical practices globally. In particular, Acinetobacter baumannii (Ab) infections are repeatedly reported as difficult to treat due to increasing antibiotic resistance. Therefore, there is increasing need to identify novel targets in the development of different antimicrobials. Of particular interest is fatty acid synthesis, vital for the formation of phospholipids, lipopolysaccharides/lipooligosaccharides, and lipoproteins of Gram-negative envelopes. The bacterial type II fatty acid synthesis (FASII) pathway is an attractive target for the development of inhibitors and is particularly favourable due to the differences from mammalian type I fatty acid synthesis. Discrete enzymes in this pathway include two reductase enzymes: 3-oxoacyl-acyl carrier protein (ACP) reductase (FabG) and enoyl-ACP reductase (FabI). Here, we investigate annotated FabG homologs, finding a low-molecular weight 3-oxoacyl-ACP reductase, as the most likely FASII FabG candidate, and high-molecular weight 3-oxoacyl-ACP reductase (HMwFabG), showing differences in structure and coenzyme preference. To date, this is the second bacterial high-molecular weight FabG structurally characterized, following FabG4 from Mycobacterium. We show that ΔAbHMwfabG is impaired for growth in nutrient rich media and pellicle formation. We also modelled a third 3-oxoacyl-ACP reductase, which we annotated as AbSDR. Despite containing residues for catalysis and the ACP coordinating motif, biochemical analyses showed limited activity against an acetoacetyl-CoA substrate in vitro. Inhibitors designed to target FabG proteins and thus prevent fatty acid synthesis may provide a platform for use against multidrug-resistant pathogens including A. baumannii.
针对“超级细菌”感染的治疗方法是创新研究的重点,因为耐药性威胁着全球人类健康和医疗实践。特别是,由于抗生素耐药性的增加,鲍曼不动杆菌(Ab)感染被反复报道为难以治疗。因此,需要在不同抗菌药物的开发中确定新的靶标。脂肪酸合成特别引人注目,因为它对革兰氏阴性包膜的磷脂、脂多糖/脂寡糖和脂蛋白的形成至关重要。细菌 II 型脂肪酸合成(FASII)途径是开发抑制剂的有吸引力的靶标,由于与哺乳动物 I 型脂肪酸合成的差异,它特别有利。该途径中的离散酶包括两种还原酶:3-氧酰基-酰基辅酶 A(ACP)还原酶(FabG)和烯酰-ACP 还原酶(FabI)。在这里,我们研究了注释的 FabG 同源物,发现低分子量 3-氧酰基-ACP 还原酶是最有可能的 FASII FabG 候选物,以及高分子量 3-氧酰基-ACP 还原酶(HMwFabG),其结构和辅酶偏好存在差异。迄今为止,这是继分枝杆菌 FabG4 之后第二个结构表征的细菌高分子量 FabG。我们表明,ΔAbHMwfabG 在营养丰富的培养基和菌膜形成中生长受损。我们还对第三种 3-氧酰基-ACP 还原酶进行了建模,我们将其注释为 AbSDR。尽管含有催化残基和 ACP 协调基序,但生化分析表明,体外对乙酰乙酰-CoA 底物的活性有限。设计用于靶向 FabG 蛋白以防止脂肪酸合成的抑制剂可能为针对包括鲍曼不动杆菌在内的多药耐药病原体提供一个平台。