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KMID : 0606920230310020141
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Biomolecules & Therapeutics
2023 Volume.31 No. 2 p.141 ~ p.147
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Structural Insights for β-Lactam Antibiotics
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Kim Dogyeoung
Kim Su-Min
Kwon Yong-Dae
Kim Ye-Seul
Park Hyun-Jae
Kwak Ki-Woong
Lee Hyeon-Min
Lee Jung-Hun
Jang Kyung-Min
Kim Dong-Hak
Lee Sang-Hee
Kang Lin-Woo
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Abstract
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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.
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KEYWORD
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Antibiotics, β-Lactams, Peptidoglycan, Antibiotic resistance, Serine β-lactamases, Metallo-β-lactamases
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