Research ArticlePain

Neurokinin 1 receptor signaling in endosomes mediates sustained nociception and is a viable therapeutic target for prolonged pain relief

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Science Translational Medicine  31 May 2017:
Vol. 9, Issue 392, eaal3447
DOI: 10.1126/scitranslmed.aal3447

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Targeting the enemy within endosomes

With opioid addiction on the rise, there is a great need for effective nonopioid approaches to treat pain. Jensen et al. examined the function of substance P neurokinin 1 receptor, which plays a role in the transmission of pain signals in the central nervous system. The authors demonstrated that endocytosis of this receptor is required for the transmission of pain signals. Although systemic inhibition of endocytosis would not be feasible in a living organism, the authors discovered another way to take advantage of this information. They conjugated neurokinin 1 receptor antagonists to cholestanol, promoting their incorporation into endosomes, where they successfully inhibited their target to block pain transmission.