BioCentury
ARTICLE | Translation in Brief

Designing specificity

How C4X Discovery identified its selective OX1R antagonist

January 4, 2018 8:04 PM UTC

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. ...