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The bacterial cell wall is an essential structural component that encases the plasma membrane, preserving cellular integrity, determining shape, and protecting against osmotic stress. This rigid yet flexible structure primarily comprises peptidoglycan, a polymer that forms a mesh-like matrix conferring mechanical strength and flexibility.Peptidoglycan Composition and StructurePeptidoglycan, the core of the bacterial cell wall, comprises alternating units of N-acetylglucosamine (NAG) and...
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Antibiotic resistance is a major public health concern that arises when bacteria evolve mechanisms to withstand the effects of antibiotic treatments. This resistance can be intrinsic, acquired through genetic mutations, or transferred between bacteria via horizontal gene transfer. The development of antibiotic resistance poses significant challenges in treating bacterial infections and necessitates ongoing research to develop new therapeutic strategies.Intrinsic resistance occurs when bacterial...
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Structure of PeptidoglycanPeptidoglycan is a vital structural component of the bacterial cell wall, providing mechanical strength and shape to the cell. It consists of repeating units of two sugars—N-acetylglucosamine (NAG) and N-acetylmuramic acid (NAM)—linked by β-1,4 glycosidic bonds. These sugar chains are cross-linked by short peptide chains, forming a mesh-like polymer that surrounds the bacterial plasma membrane.Cytoplasmic Phase – Precursor SynthesisPeptidoglycan...
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The Use of a &#946;-lactamase-based Conductimetric Biosensor Assay to Detect Biomolecular Interactions
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Structural Insights for β-Lactam Antibiotics.

Dogyeoung Kim1, Sumin Kim1, Yongdae Kwon1

  • 1Department of Biological Sciences, Konkuk University, Seoul 05029, Republic of Korea.

Biomolecules & Therapeutics
|February 15, 2023
PubMed
Summary
This summary is machine-generated.

Antibiotic resistance is a major global health threat. This review details the 3D structures of beta-lactam antibiotics, aiding in understanding their efficacy and developing new drugs against resistant bacteria.

Keywords:
Antibiotic resistanceAntibioticsMetallo-β-lactamasesPeptidoglycanSerine β-lactamasesβ-Lactams

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Area of Science:

  • Medicinal Chemistry
  • Microbiology
  • Structural Biology

Background:

  • Antibiotic resistance poses a significant global health challenge, diminishing the effectiveness of many antimicrobial agents.
  • Beta-lactam antibiotics are widely prescribed, representing about two-thirds of the antibiotic market.
  • These antibiotics function by inhibiting bacterial cell wall synthesis, specifically the peptidoglycan layer.

Purpose of the Study:

  • To review the three-dimensional structural characteristics of beta-lactam antibiotics.
  • To elucidate the relationship between structure, mechanism of action, and resistance.
  • To guide the development of novel beta-lactam antibiotics and inhibitors.

Main Methods:

  • Review of existing literature on beta-lactam antibiotic structures.
  • Analysis of structural data concerning scaffolds, chemical diversity, and hydrolysis by beta-lactamases.
  • Examination of structure-activity relationships and resistance mechanisms.

Main Results:

  • Detailed examination of the three-dimensional scaffolds of various beta-lactam antibiotics.
  • Understanding of how structural features influence antibacterial efficacy and susceptibility to resistance.
  • Insights into the hydrolysis mechanisms mediated by beta-lactamases.

Conclusions:

  • Structural understanding is crucial for combating antibiotic resistance.
  • Knowledge of beta-lactam structures can inform the design of new antibiotics effective against multidrug-resistant bacteria.
  • Further research into beta-lactam structures and their interactions with resistance enzymes is warranted.