Mechanism of inhibition of ASIC1a by the antiprotozoal drug diminazene revealed

What is it about?

Activation of Acid-sensing ion channels (ASICs) contributes, among others, to neurodegeneration after ischemic stroke and pathological pain, for example neuropathic pain. Due to their pathophysiological importance inhibitors of ASICs are clinically relevant. A relatively new inhibitor of ASICs is diminazene, a drug that is used in veterinary medicine to treat infections with protozoans. We found that diminazene inhibits ASICs by slowly binding into the ion pore. Additionally, we identify by a combination of functional and computational methods in detail the binding site of diminazene in the ASIC pore.

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Why is it important?

Our results are useful for developing high-affinity inhibitors of ASICs, that are based on diminazene.