Crystal structure of the human NK₁ tachykinin receptor.

ABSTRACT: The NK₁ tachykinin G-protein-coupled receptor (GPCR) binds substance P, the first neuropeptide to be discovered in mammals. Through activation of NK₁R, substance P modulates a wide variety of physiological and disease processes including nociception, inflammation, and depression. Human NK₁R (hNK₁R) modulators have shown promise in clinical trials for migraine, depression, and emesis. However, the only currently approved drugs targeting hNK₁R are inhibitors for chemotherapy-induced nausea and vomiting (CINV). To better understand the molecular basis of ligand recognition and selectivity, we solved the crystal structure of hNK₁R bound to the inhibitor L760735, a close analog of the drug aprepitant. Our crystal structure reveal

SUBMITTER: Yin J 

PROVIDER: S-EPMC6310836 | biostudies-literature | 2018 Dec

REPOSITORIES: biostudies-literature