Structure-based drug discovery of carbonic anhydrase inhibitors

University of Florence

PubMed
Indexed incrossrefdoajpubmed

Abstract

Inhibition of the metalloenzyme carbonic anhydrase (CA; EC 4.2.1.1) has pharmacologic applications in the field of anti-glaucoma, anti-convulsant and anti-cancer agents. But recently, it has also emerged that these enzymes have the potential for designing anti-infective drugs (anti-fungal and anti-bacterial agents) with a novel mechanism of action. Sulphonamides and their isosteres (sulphamates/sulphamides) constitute the main class of CA inhibitors (CAIs), which bind to the metal ion from the enzyme active site. Recently, the dithiocarbamates (DTCs), possessing a similar mechanism of action, were reported as a new class of inhibitors. These types of CAIs will be discussed in detail in this review. Novel drug…

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Authors

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Topics & keywords

Keywords
  • Carbonic anhydrase
  • Chemistry
  • Enzyme
  • Active site
  • Mechanism of action
  • Druggability
  • Drug
  • Combinatorial chemistry
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