N‑myristoyltransferase inhibitors as a potential starting point for the development of antischistosomal agents
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Abstract
Schistosomiasis remains a major global health challenge, and the threat of emerging praziquantel resistance highlights the need for new therapeutic strategies. Here, the Schistosoma mansoni N-myristoyltransferase was evaluated as a potential drug target. Six reported NMT inhibitors were tested for SmNMT inhibition and binding, with two compounds showing low nanomolar potency. These also inhibited NMT of S. hematobium and S. japonicum, and exhibit favorable drug-like physicochemical properties. In addition, antiparasitic activity against newly transformed schistosomula and adult worms was investigated. The results confirm NMT as a viable target for drug discovery against schistosomiasis and provide a basis for further optimizations of SmNMT inhibitors.
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ACS medicinal chemistry letters, 17, 4, ACS, Washington, DC, 2026, https://doi.org/10.1021/acsmedchemlett.6c00145