12:04 PM
Jan 04, 2018
 |  BC Innovations  |  Translation in Brief

Designing specificity

How C4X Discovery identified its selective OX1R antagonist

Solving a key problem in the orexin field, C4X Discovery Holdings plc (LSE:C4XD) has described how its technology platform yielded an antagonist with selectivity for OX1R over OX2R and disclosed data for the compound in a preclinical model of addiction.

The orexin system consists of two isoforms of orexin (hypocretin; HCRT) -- orexin-A and orexin-B -- that bind the G protein-coupled receptors orexin 1 receptor (OX1R; HCRTR1) and OX2R (HCRTR2). Previous studies have shown roles for OX1R-expressing neurons in reward-seeking behavior and anxiety response, and for OX2R in sleep regulation.

According to CEO Clive Dix, the OX1R pathway has attracted attention because “there are very few other pathways that are very clearly established as areas for addiction.”

However, the development of selective OX1R antagonists...

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