Dogyeoung Kim, Sumin Kim, Yongdae Kwon, Yeseul Kim, Hyunjae Park, Kiwoong Kwak, Hyeonmin Lee, Jung Hun Lee, Kyung-Min Jang, Donghak Kim, Sang Hee Lee, Lin-Woo Kang
Author Information
Dogyeoung Kim: Department of Biological Sciences, Konkuk University, Seoul 05029, Republic of Korea.
Sumin Kim: Department of Biological Sciences, Konkuk University, Seoul 05029, Republic of Korea.
Yongdae Kwon: Department of Biological Sciences, Konkuk University, Seoul 05029, Republic of Korea.
Yeseul Kim: Department of Biological Sciences, Konkuk University, Seoul 05029, Republic of Korea.
Hyunjae Park: Department of Biological Sciences, Konkuk University, Seoul 05029, Republic of Korea.
Kiwoong Kwak: Department of Biological Sciences, Konkuk University, Seoul 05029, Republic of Korea.
Hyeonmin Lee: Department of Biological Sciences, Konkuk University, Seoul 05029, Republic of Korea.
Jung Hun Lee: National Leading Research Laboratory of Drug Resistance Proteomics, Department of Biological Sciences, Myongji University, Yongin 17058, Republic of Korea.
Kyung-Min Jang: National Leading Research Laboratory of Drug Resistance Proteomics, Department of Biological Sciences, Myongji University, Yongin 17058, Republic of Korea.
Donghak Kim: Department of Biological Sciences, Konkuk University, Seoul 05029, Republic of Korea.
Sang Hee Lee: National Leading Research Laboratory of Drug Resistance Proteomics, Department of Biological Sciences, Myongji University, Yongin 17058, Republic of Korea.
Lin-Woo Kang: Department of Biological Sciences, Konkuk University, Seoul 05029, Republic of Korea.
Antibiotic resistance has emerged as a global threat to modern healthcare systems and has nullified many commonly used antibiotics. β-Lactam antibiotics are among the most successful and occupy approximately two-thirds of the prescription antibiotic market. They inhibit the synthesis of the peptidoglycan layer in the bacterial cell wall by mimicking the D-Ala-D-Ala in the pentapeptide crosslinking neighboring glycan chains. To date, various β-lactam antibiotics have been developed to increase the spectrum of activity and evade drug resistance. This review emphasizes the three-dimensional structural characteristics of β-lactam antibiotics regarding the overall scaffold, working mechanism, chemical diversity, and hydrolysis mechanism by β-lactamases. The structural insight into various β-lactams will provide an in-depth understanding of the antibacterial efficacy and susceptibility to drug resistance in multidrug-resistant bacteria and help to develop better β-lactam antibiotics and inhibitors.