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Antimicrobial Peptides Produced by Selective Pressure Incorporation of Non-canonical Amino Acids
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Advances in Bacterial Methionine Aminopeptidase Inhibition

Travis R Helgren, Phumvadee Wangtrakuldee, Bart L Staker

  • 1Northern Illinois University, Department of Chemistry and Biochemistry, DeKalb, IL 60115 USA. thagen@niu.edu.

Current Topics in Medicinal Chemistry
|August 14, 2015
PubMed

Insights

Methionine aminopeptidases (MetAPs) are essential bacterial enzymes and potential drug targets. Structural analysis reveals differences between bacterial and human MetAPs, guiding the development of selective antibacterial agents.

Area of Science:

  • Biochemistry
  • Structural Biology
  • Medicinal Chemistry

Background:

  • Methionine aminopeptidases (MetAPs) are essential metalloenzymes in bacteria, crucial for protein synthesis.
  • MetAP activity is vital for bacterial survival, identifying them as promising antibacterial drug targets.
  • Human MetAPs share structural similarities, necessitating selective inhibition strategies.

Purpose of the Study:

  • To review crystallographic data of bacterial MetAPs.
  • To compare bacterial and human MetAP structures for selectivity insights.
  • To analyze the chemical diversity of bacterial MetAP inhibitors.

Main Methods:

  • Crystallographic data analysis of bacterial MetAPs.
  • Comparative structural analysis between bacterial and human MetAPs.
  • Review of chemical inhibitors targeting bacterial MetAPs.

Main Results:

  • Over 65 bacterial MetAP crystal structures are available in the PDB.
  • Structural differences between bacterial and human MetAPs identified.
  • Diverse chemical scaffolds inhibit bacterial MetAP enzymes.

Conclusions:

  • Bacterial MetAPs represent a viable target for novel antibacterial drug development.
  • Structural comparisons facilitate the design of selective inhibitors.
  • Understanding inhibitor chemical space aids in developing effective antibacterial agents.

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