Centre for Bio-Separation Technology, Vellore Institute of Technology, Vellore, Tamil Nadu 632014, India.
Int J Biol Macromol. 2023 Apr 15;234:122960. doi: 10.1016/j.ijbiomac.2022.12.179. Epub 2022 Dec 22.
Microbial infections are becoming resistant to traditional antibiotics. As novel resistance mechanisms are developed and disseminated across the world, our ability to treat the most common infectious diseases is becoming increasingly compromised. As existing antibiotics are losing their effectiveness, especially treatment of bacterial infections, is difficult. In order to combat this issue, it is of utmost importance to identify novel pharmacological targets or antibiotics. LpxC, a zinc-dependent metalloamidase that catalyzes the committed step in the biosynthesis of lipid A (endotoxin) in bacteria, is a prime candidate for drug/therapeutic target. So far, the rate-limiting metallo-amidase LpxC has been the most-targeted macromolecule in the Raetz pathway. This is because it is important for the growth of these bacterial infections. This review showcases on the research done to develop efficient drugs in this area before and after the 2015.
微生物感染对传统抗生素的耐药性日益增强。随着新的耐药机制在全球范围内的发展和传播,我们治疗最常见传染病的能力受到了越来越大的影响。由于现有抗生素的有效性正在逐渐丧失,尤其是对细菌感染的治疗变得更加困难。为了解决这个问题,确定新的药理学靶点或抗生素至关重要。LpxC 是一种锌依赖性金属酰胺酶,它催化细菌中脂质 A(内毒素)生物合成的关键步骤,是药物/治疗靶点的首选候选物。到目前为止,限速金属酰胺酶 LpxC 一直是雷茨途径中最受关注的大分子。这是因为它对这些细菌感染的生长很重要。这篇综述展示了在 2015 年前后在这一领域开发有效药物的研究进展。