Researchers at the Institute for Molecular Bioscience (IMB) at The University of Queensland (UQ) have developed a novel peptide-based inhibitor of the acid sensing ion channel isoform 1a (ASIC1a). ASICs are members of the epithelial sodium channel/degererin family of receptors and are activated by decreases in intracellular pH. Alternative splicing of four ASIC-encoding genes leads to the expression of six subunits (ASIC1a, ASIC1b, ASIC2a, ASIC2b, ASIC3,and ASIC4) that combine to form hetero- or homotrimericchannels that differ in their pH sensitivity, kinetics, and susceptibility to desensitisation. Postsynaptic ASIC1a channels are the dominant ASIC subtype in both human and rodent brain and have been implicated in a number of diseases, including stroke.
Therapeutic applications of the ASIC1a inhibitor include:
- Neuroprotection following stroke;
- Migraine and chronic pain;
- Multiple sclerosis; and
- Neurodegenerative disorders such as Huntington’s and Parkinson’s disease.