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Classical and New Pharmaceutical Uses of Bacterial Penicillin G Acylase

机译:细菌青霉素G acylase的古典和新的药物用途

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Background: beta-lactam antibiotics are the most used worldwide for the treatment of bacterial infections. The consumption of these classes of drugs is high, and it is increasing around the world. To date, the best way to produce them is using penicillin G Acylase (PGA) as a biocatalyst.Objective: This manuscript offers an overview of the most recent advances in the current tools to improve the activity of the PGA and its pharmaceutical application.Results: Several microorganisms produce PGA, but some bacterial strains represent the primary source of this enzyme. The activity of bacterial PGA depends on its adequate expression and carbon or nitrogen source, as well as a specific pH or temperature depending on the nature of the PGA. Additionally, the PGA activity can be enhanced by immobilizing it to a solid support to recycle it for a prolonged time. Likewise, PGAs more stable and with higher activity are obtained from bacterial hosts genetically modified.Conclusion: PGA is used to produce b-lactam antibiotics. However, this enzyme has pharmaceutical potential to be used to obtain critical molecules for the synthesis of anti-tumor, antiplatelet, antiemetic, antidepressive, anti-retroviral, antioxidant, and antimutagenic drugs.
机译:背景:β-内酰胺抗生素是全世界最使用的,用于治疗细菌感染。这些课程的消费量很高,而且在世界各地正在增加。迄今为止,生产它们的最佳方法是使用青霉素G acylase(PGA)作为生物催化剂。该手稿概述了当前工具中最新进展的概述,以改善PGA的活动及其制药应用。结果:几种微生物产生PGA,但一些细菌菌株代表该酶的主要来源。细菌PGA的活性取决于其足够的表达和碳或氮源,以及根据PGA的性质,以及特定的pH或温度。另外,通过将其固定到固体载体来再循环延长时间,可以增强PGA活性。同样,PGA从遗传修饰的细菌宿主获得更稳定和更高的活性。结论:PGA用于生产B-内酰胺抗生素。然而,该酶具有用于获得抗肿瘤,抗血小板,抗抑化,抗抑郁,抗逆转录病毒,抗氧化剂和抗微生物药物的临界分子的药物潜力。

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