Suramin is over 100 years old and is still used to treat Human African trypanosomiasis, caused by Trypanosoma brucei rhodesiense. It is a multifunctional molecule with a wide array of potential applications, from parasitic and viral diseases to cancer, snakebite and autism spectrum disorder. It is offered by AdipoGen Life Sciences and distributed in Australia and New Zealand by Sapphire Bioscience.
Suramin is a large molecule that carries six negative charges at physiological pH that binds to and therefore inhibits various proteins, as many enzymes have been shown to be inhibited by suramin. Suramin inhibits many glycolytic enzymes; decreases the activities of many enzymes involved in DNA and RNA synthesis and modification; inhibits histone- and chromatin-modifying enzymes; and is also an inhibitor of other sirtuins and protein kinases, phospholipase A2, protein tyrosine phosphatases, and different serine and cysteine proteases. It further inhibits the Na+, K+-ATPase and other ATPases, certain GABA receptors classes and several G protein-coupled receptors.
Suramin has showed inhibitory effects against components of the coagulation cascade and the complement system, and against deubiquitinating enzymes. Besides its many inhibitory activities, it activates certain nuclear receptors that act as transcription factors and intracellular calcium channels. Most recently, suramin has been shown to be an effective inhibitor of dsDNA-induced inflammation, several dsDNA-binding proteins, Mcm1040, DNA topoisomerase II and the AIM2 inflammasome. Suramin inhibits AIM2-dependent ASC oligomerisation, caspase-1 and IL-1β processing, and is a clinical drug that reversibly inhibits the AIM2 inflammasome in humans and mice.
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