Microbiology Department, Research Institute Biomedical A Coruña (INIBIC), Hospital A Coruña (CHUAC), University of A Coruña (UDC), A Coruña, Spain.
National Infection Service Laboratories, Public Health England, Colindale, United Kingdom.
Antimicrob Agents Chemother. 2020 Sep 21;64(10). doi: 10.1128/AAC.01283-20.
Antibiotic failure not only is due to the development of resistance by pathogens but can also often be explained by persistence and tolerance. Persistence and tolerance can be included in the "persistent phenotype," with high relevance for clinics. Two of the most important molecular mechanisms involved in tolerance and persistence are toxin-antitoxin (TA) modules and signaling via guanosine pentaphosphate/tetraphosphate [(p)ppGpp], also known as "magic spot." (p)ppGpp is a very important stress alarmone which orchestrates the stringent response in bacteria; hence, (p)ppGpp is produced during amino acid or fatty acid starvation by proteins belonging to the RelA/SpoT homolog family (RSH). However, (p)ppGpp levels can also accumulate in response to a wide range of signals, including oxygen variation, pH downshift, osmotic shock, temperature shift, or even exposure to darkness. Furthermore, the stringent response is not only involved in responses to environmental stresses (starvation for carbon sources, fatty acids, and phosphates or heat shock), but it is also used in bacterial pathogenesis, host invasion, and antibiotic tolerance and persistence. Given the exhaustive and contradictory literature surrounding the role of (p)ppGpp in bacterial persistence, and with the aim of summarizing what is known so far about the magic spot in this bacterial stage, this review provides new insights into the link between the stringent response and persistence. Moreover, we review some of the innovative treatments that have (p)ppGpp as a target, which are in the spotlight of the scientific community as candidates for effective antipersistence agents.
抗生素治疗失败不仅是由于病原体产生了耐药性,还常常可以归因于持久性和耐受性。持久性和耐受性可以包含在“持久表型”中,这与临床密切相关。与耐受性和持久性相关的两个最重要的分子机制是毒素-抗毒素 (TA) 模块和鸟苷五磷酸/四磷酸 [(p)ppGpp] 信号转导,也称为“魔点”。(p)ppGpp 是一种非常重要的应激警报素,它在细菌中协调严谨反应;因此,(p)ppGpp 是由 RelA/SpoT 同源家族 (RSH) 蛋白在氨基酸或脂肪酸饥饿时产生的。然而,(p)ppGpp 水平也可以在响应广泛的信号时积累,包括氧气变化、pH 值下降、渗透压冲击、温度变化,甚至暴露在黑暗中。此外,严谨反应不仅参与对环境应激(碳源、脂肪酸和磷酸盐饥饿或热休克)的反应,还参与细菌发病机制、宿主入侵以及抗生素耐受性和持久性。鉴于围绕 (p)ppGpp 在细菌持久性中的作用的文献详尽且相互矛盾,并且为了总结迄今为止关于细菌阶段中魔点的已知信息,本综述提供了关于严谨反应和持久性之间联系的新见解。此外,我们还回顾了一些将 (p)ppGpp 作为靶点的创新治疗方法,这些方法作为有效的抗持久药物候选物受到科学界的关注。