BioCentury
ARTICLE | Translation in Brief

Pockets against pain

Amgen fills an allosteric pocket in GLRA3 to dampen neuropathic pain

January 19, 2017 5:57 PM UTC

Amgen Inc. (NASDAQ:AMGN) is aiming to tackle neuropathic pain by boosting glycine receptor α 3 (GLRA3) activity in the CNS. In a December study, the company presented preclinical data and crystal structures for its GLRA3 positive allosteric modulators (PAMs) that pointed to a new druggable pocket in the target.

Upon glycine binding, GLRA3 triggers chloride ion currents, which mediate inhibitory neurotransmission that dampens pain signals. Jacinthe Gingras, a senior scientist in neuroscience at Amgen and author on the study, told BioCentury that glycine receptors have been recognized as potential pain targets for over a decade, but have been passed over by drug developers so far in favor of lower-hanging fruit that doesn’t have to cross the blood-brain barrier...

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