NK1R, Active Human Recombinant GPCR

The human neurokinin-1 receptor (NK1R) is a class A G protein–coupled receptor (GPCR) that binds the neuropeptide substance P with high affinity. This recombinant form corresponds to the full-length human NK1R, expressed in HEK293F cells and purified under native conditions using StrepTactin affinity chromatography followed by size-exclusion chromatography. The receptor includes an N-terminal His₁₀ and Twin-Strep tag, enabling affinity-based detection or optional repurification after functional use. Its activity has been validated through ligand-binding assays using aprepitant, a selective NK1R antagonist, confirming correct folding and pharmacological relevance. Expression in mammalian cells ensures proper post-translational modifications and membrane integration, critical for maintaining native conformation and functionality. The protein is solubilized in a detergent system compatible with biochemical and structural applications, including receptor reconstitution and cryo-EM. NK1R is involved in numerous physiological and pathological processes, including pain transmission, neurogenic inflammation, stress response, emesis, and cancer progression. Its clinical relevance and validated activity make this recombinant form a robust tool for drug discovery and mechanistic studies.