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Biochemical and Structural Characterization of the Carbohydrate Transport Substrate-binding-protein SP0092
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Penicillin binding protein 2a: An overview and a medicinal chemistry perspective

Menna-Allah W Shalaby1, Eman M E Dokla1, Rabah A T Serya1

  • 1Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ain Shams University, Abbassia, 11566, Cairo, Egypt.

European Journal of Medicinal Chemistry
|May 23, 2020
PubMed

Insights

Methicillin-resistant Staphylococcus aureus (MRSA) poses a global threat due to its resistance. Targeting the PBP2a enzyme offers a promising strategy to inhibit bacterial cell wall biosynthesis and combat MRSA infections.

Area of Science:

  • Microbiology
  • Infectious Diseases
  • Drug Discovery

Background:

  • Antimicrobial resistance is a significant global health challenge.
  • Methicillin-resistant Staphylococcus aureus (MRSA) is a major pathogen responsible for difficult-to-treat infections.
  • MRSA confers resistance primarily through the production of penicillin-binding protein 2a (PBP2a).

Purpose of the Study:

  • To review the role of PBP2a in MRSA resistance.
  • To examine existing and novel therapeutic strategies targeting PBP2a.
  • To discuss future perspectives for combating MRSA infections.

Main Methods:

  • Literature review of scientific publications on MRSA and PBP2a.
  • Analysis of the biochemical mechanisms of PBP2a in conferring resistance.
  • Evaluation of the therapeutic potential of PBP2a inhibitors.

Main Results:

  • PBP2a's low affinity for beta-lactam antibiotics is a key mechanism of MRSA resistance.
  • PBP2a is a validated target for developing new antimicrobial agents.
  • Several classes of antibiotics and novel compounds targeting PBP2a have shown therapeutic promise.

Conclusions:

  • Inhibition of PBP2a is a viable strategy to overcome MRSA resistance.
  • Further research into PBP2a-targeting agents is crucial for developing effective treatments.
  • Targeting PBP2a holds significant potential for future MRSA infection management.
Keywords:
Allosteric controlAnti-MRSAAntimicrobial resistanceEnzyme inhibitorPenicillin binding protein 2aβ-lactams

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