• Title/Summary/Keyword: biological sciences

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Structural Insights for β-Lactam Antibiotics

  • 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
    • Biomolecules & Therapeutics
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    • v.31 no.2
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    • pp.141-147
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    • 2023
  • 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.