Fighting pain: the structure of gabapentin and its binding site in the Ca-v alpha(2)delta subunit

Gabapentinoids are first-line treatments for chronic pain but are associated with adverse side effects. A cryo-EM structure of gabapentin bound to its interaction site on the calcium channel alpha(2)delta subunit now paves the way for the rational design of analgesics with greater selectivity and a reduced potential for adverse effects.