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Suramin is a polysulfonated naphthylurea with antiviral, antiparasitic, and anticancer activities.1 It is negatively charged at physiological pH and, therefore, binds to various intracellular targets including, but not limited to, ryanodine receptor 1 (IC50 = 4.9 µM), G protein-coupled receptors, purinergic P2 receptors, PDGF, PKC, transferrin, DNA and RNA polymerases, sirtuins, and various cytokines.1,2,3 It reduces Zika virus infectivity in Vero cells (IC50 = ~2.5-5 µg/ml).4 Suramin reduces the proliferation of bloodstream forms of T. brucei (MIC = 0.1 µM).5 It also neutralizes the myotoxic effect of the basic phospholipase A2 (PLA2) homolog MjTX-I, a Lys49-PLA2 protein from snake venom, in mouse phrenic-diaphragm preparations.6 Suramin (60 mg/kg) reduces tumor volume in patient-derived xenograft (PDX) mouse models of malignant mesothelioma.7 Formulations containing suramin have been used in the treatment of African sleeping sickness.
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1. 100 years of suramin. Antimicrob. Agents Chemother. 64(3), e01168-01119 (2020).
2. Suramin and the suramin analogue NF307 discriminate among calmodulin-
3. PPADS and suramin as antagonists at cloned P2Y-
4. Polysulfonate suramin inhibits Zika virus infection. Antiviral Res. 143, 186-194 (2017).
5. Suramin: Effectiveness of analogues reveals structural features that are important for the potent trypanocidal activity of the drug. Exp. Parasitol. 260, 108744 (2024).
6. Structural and functional characterization of suramin-
7. Effectiveness of cisplatin, paclitaxel, and suramin against human malignant mesothelioma xenografts in athymic nude mice. J. Surg. Oncol. 67(2), 104-111 (1998).