Dual targeting carbonic anhydrase inhibitors as promising therapeutic approach: a structural overview

Katia D'Ambrosio1, Anna Di Fiore1, Emma Langella1

  • 1Institute of Biostructures and Bioimaging - CNR, Napoli, Italy.

PubMed

Insights

Dual-target inhibitors offer a promising strategy for complex diseases by targeting multiple pathways. Human carbonic anhydrase inhibitors are explored for dual-targeting to enhance drug efficacy and combat resistance.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Dual-target inhibitor strategies address multifactorial diseases like cancer, inflammation, and neurological disorders.
  • These strategies enhance therapeutic outcomes, minimize side effects, and prevent drug resistance by targeting multiple disease pathways.
  • Human carbonic anhydrases (hCAs) are validated targets due to their roles in pH balance, ion transport, and fluid regulation, with dysregulation linked to various pathologies.

Purpose of the Study:

  • To review structural findings in the development of novel therapeutics using dual-targeting strategies.
  • To highlight the potential of human carbonic anhydrase inhibitors in dual-targeting drug development for complex diseases.

Main Methods:

  • Literature review focusing on structural biology and medicinal chemistry of dual-target inhibitors.
  • Analysis of studies involving human carbonic anhydrases as a component of dual-targeting approaches.

Main Results:

  • Identification of human carbonic anhydrases as suitable targets for dual-inhibitor design.
  • Exploration of structural insights for developing novel therapeutics that combine hCA inhibition with modulation of a second target.

Conclusions:

  • Dual-targeting inhibitors, particularly those involving hCAs, represent a promising therapeutic avenue for complex diseases.
  • Further structural studies are crucial for designing effective dual-targeting drugs with improved efficacy and reduced resistance.

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