| 摘要: |
| 青霉素G酰化酶是近几十年来β内酰胺类抗生素领域应用最广、开发最成功的酶之一。伴随着β-内酰胺类抗生素由化学合成法变更为酶法在中国的大规模产业化，得到了充分的开发与应用，取得了成功。青霉素G酰化酶不但用于水解制备6-APA、7-ADCA，更重要的是用于氨苄西林、头孢氨苄、阿莫西林、头孢拉定、头孢克洛等抗生素的制备。本文综述了近15年青霉素G酰化酶在我国研究与应用的历史沿革、基因与蛋白质结构、工业应用表达体系、工业评价标准与进化研究，还对各种突变株在具体医药工业领域的开发应用进行了综述，旨在梳理青霉素G酰化酶结构与性能的进化趋势以及在医药工业领域取得的巨大成就，同时也为相关人员在此领域进行深耕提供参考。 |
| 关键词: 青霉素G酰化酶 6-APA 抗生素 突变体 进化 |
| DOI：10.14188/j.ajsh.2023.05.003 |
| 分类号:Q814 |
| 基金项目:河北省高校应用技术研发中心平台项目（2020-4） |
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| Research progress in the industrial evolution of penicillin G acylase |
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REN Limei1,2,3, WANG Xiaoru1,2,3, QI Yonghao1, HAN Guangxin1, LI Xiaobing1,2,3
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1.Department of Chemical Engineering， Shijiazhuang University， Shijiazhuang 050035， Hebei， China;2.Hebei Provincial University Microbiology Pharmaceutical Application Technology Research and Development Center， Shijiazhuang University， Shijiazhuang 050035， Hebei， China;3.Hebei International Joint Research Center for Biopharmaceutical， Shijiazhuang University， Shijiazhuang 050035， Hebei， China
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| Abstract: |
| Penicillin G acylase （PGA） is one of the most widely used and successfully developed enzymes in the field of β-lactam antibiotics in recent decades. In China， along with the large-scale industrialization of β-lactam antibiotics，chemical synthesis methods to enzymatic methods， PGA have been fully developed and applied， and achieved success. Penicillin G acylase is not only used for hydrolysis to prepare 6-APA and 7-ADCA， but also for semisynthetic antibiotics such as ampicillin， cephalexin， amoxicillin， cefradine and cefaclor. This paper reviews the history， gene and protein structure， industrial expression system， industrial evaluation criteria and evolution of penicillin G acylase research and application in China in the past 15 years. At the same time， the development and application of various mutants of penicillin G acylase in specific pharmaceutical industry fields are also reviewed， aiming to sort out the evolution trend of the structure and performance of penicillin G acylase， its great achievements in the pharmaceutical industry field， and point out the direction for related researchers to delve deeper in this field. |
| Key words: penicillin G acylase 6-APA antibiotic mutant evolution |
