Dear Colleagues,

Natural products represent a huge source of therapeutic agent collections, and, historically, they have proven to be an effective way to access chemical diversity for lead-generation in drug discovery strategies. There is currently a renewed interest in natural products due to the urgent need for new drugs, especially in some pathologies, such as cancer and bacterial infections.

Carbonic anhydrases (CA, EC 4.2.1.1), which belong to the lyase family, are zinc metalloenzymes of medical relevance, present in prokaryotes and eukaryotes. They are efficient catalysts for the hydration of carbon dioxide to bicarbonate and protons, playing crucial physiological/pathological roles in acid–base homeostasis, secretion of electrolytes, transport of ions, biosynthetic reactions, and tumorigenesis.

These enzymes are of clinical relevance, as some catalytically active isoforms in humans are established drug targets, with many inhibitors that have already demonstrated a crucial therapeutic potential in various pathological situations, especially as diuretics, antiglaucoma, anticancer, or for the management of a variety of neurological disorders, including epilepsy and altitude disease.

Even if the synthetic source of carbonic anhydrase is very large, there is always a need for the discovery of specific CA inhibitors that can discriminate between two different families (such as for example human -CAs and bacterial -CAs) or between the different isoforms in the same CA family.

Recent preliminary studies have shown that natural sources of compounds, derived from either plants or fungi, have disclosed novel chemotypes possessing carbonic anhydrase inhibition activities. The revival of interest in natural products, thus, offers new opportunities in the search for new and more effective carbonic anhydrase inhibitors against human isoforms, and also bacterial carbonic anhydrases, and may serve as new leads in the design and development of drugs.

This Special Issue is dedicated to recent advances in the search of naturally occurring products and their synthetic derivatives, which can inhibit the CAs, their mechanisms of action, and their potential medical applications. Original papers, reviews articles and perspectives from experts in the field are welcome.

Dr. Jean-Yves Winum
Guest Editor

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• natural products
• carbonic anhydrases
• isoforms
• metalloenzyme
• inhibitors
• drug discovery
• drug design
• chemotypes
• synthetic derivatives
• therapeutic applications
• crystal structure
• mechanism of action