ArticleActa crystallographica. Section D, Structural biology2022
Inhibition of Schistosoma mansoni carbonic anhydrase by the antiparasitic drug clorsulon: X-ray crystallographic and in vitro studies.
Article in Acta crystallographica. Section D, Structural biology, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 13 citations in OpenAlex.
- Tetrazole Is a Novel Zinc Binder Chemotype for Carbonic Anhydrase Inhibition.ACS medicinal chemistry letters · 2025Article
- Potency of anti-trematode in inhibiting cathepsin-2L and cathepsin-5L ofOpen veterinary journal · 2024Article
- Sulphonamide inhibition studies of the β-carbonic anhydrase GsaCAβ present in the salmon platyhelminth parasiteJournal of enzyme inhibition and medicinal chemistry · 2023Article
- Cloning, characterization, and inhibition of the novel β-carbonic anhydrase from parasitic blood fluke,Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Anthelmintic potential of sulphonamides andJournal of parasitic diseases : official organ of the Indian Society for Parasitology · 2023Article
- Role of the Abcg2 Transporter in Secretion into Milk of the Anthelmintic Clorsulon: Interaction with Ivermectin.Antimicrobial agents and chemotherapy · 2023Article
- Cloning, purification, kinetic and anion inhibition studies of a recombinant β-carbonic anhydrase from the Atlantic salmon parasite platyhelminthJournal of enzyme inhibition and medicinal chemistry · 2022Article
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
Clorsulon is an anthelmintic drug that is clinically used against Fasciola hepatica. Due to the presence of two sulfonamide moieties in its core nucleus, which are well recognized as zinc-binding groups, it was proposed that it may be efficacious in the inhibition of parasite carbonic anhydrases (CAs). Proteomic analyses revealed the presence of CA in the tegument of Schistosoma mansoni, and recently the druggability of this target was explored by testing the inhibitory activities of several sulfonamide-based derivatives. According to the principles of drug repurposing, the aim was to demonstrate a putative new mechanism of action of clorsulon and thus widen its antiparasitic spectrum. For this purpose, the inhibitory activity and isoform selectivity of clorsulon was studied using human CA I and S. mansoni CA, revealing different modes of binding of clorsulon that explain its inhibitory potency against the two enzymes. The information obtained in this study could be crucial in the design of more active and selective derivatives.
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Registered trials
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