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Identification of an allosteric binding site on the human glycine transporter, GlyT2, for bioactive lipid analgesics

Mostyn, Shannon; Wilson, Katie; Schumann-Gillett, Alexandra; Frangos, Zachary J; Shimmon, Susan; Rawling, Tristan; Ryan, Renae M.; O'Mara, Megan; Vandenberg, Robert J

Description

The treatment of chronic pain is poorly managed by current analgesics, and there is a need for new classes of drugs. We recently developed a series of bioactive lipids that inhibit the human glycine transporter GlyT2 (SLC6A5) and provide analgesia in animal models of pain. Here, we have used functional analysis of mutant transporters combined with molecular dynamics simulations of lipid-transporter interactions to understand how these bioactive lipids interact with GlyT2. This study...[Show more]

CollectionsANU Research Publications
Date published: 2019
Type: Journal article
URI: http://hdl.handle.net/1885/211064
Source: eLife
DOI: 10.7554/eLife.47150
Access Rights: Open Access

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