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A lipid-anchored neurokinin 1 receptor antagonist prolongs pain relief by a three-pronged mechanism of action targeting the receptor at the plasma membrane and in endosomes.
Mai QN, Shenoy P, Quach T, Retamal JS, Gondin AB, Yeatman HR, Aurelio L, Conner JW, Poole DP, Canals M, Nowell CJ, Graham B, Davis TP, Briddon SJ, Hill SJ, Porter CJH, Bunnett NW, Halls ML, Veldhuis NA. Mai QN, et al. J Biol Chem. 2021 Jan-Jun;296:100345. doi: 10.1016/j.jbc.2021.100345. Epub 2021 Jan 28. J Biol Chem. 2021. PMID: 33515548 Free PMC article.
A pH-responsive nanoparticle targets the neurokinin 1 receptor in endosomes to prevent chronic pain.
Ramírez-García PD, Retamal JS, Shenoy P, Imlach W, Sykes M, Truong N, Constandil L, Pelissier T, Nowell CJ, Khor SY, Layani LM, Lumb C, Poole DP, Lieu T, Stewart GD, Mai QN, Jensen DD, Latorre R, Scheff NN, Schmidt BL, Quinn JF, Whittaker MR, Veldhuis NA, Davis TP, Bunnett NW. Ramírez-García PD, et al. Among authors: mai qn. Nat Nanotechnol. 2019 Dec;14(12):1150-1159. doi: 10.1038/s41565-019-0568-x. Epub 2019 Nov 4. Nat Nanotechnol. 2019. PMID: 31686009 Free PMC article.
Neurokinin 1 receptor signaling in endosomes mediates sustained nociception and is a viable therapeutic target for prolonged pain relief.
Jensen DD, Lieu T, Halls ML, Veldhuis NA, Imlach WL, Mai QN, Poole DP, Quach T, Aurelio L, Conner J, Herenbrink CK, Barlow N, Simpson JS, Scanlon MJ, Graham B, McCluskey A, Robinson PJ, Escriou V, Nassini R, Materazzi S, Geppetti P, Hicks GA, Christie MJ, Porter CJH, Canals M, Bunnett NW. Jensen DD, et al. Among authors: mai qn. Sci Transl Med. 2017 May 31;9(392):eaal3447. doi: 10.1126/scitranslmed.aal3447. Sci Transl Med. 2017. PMID: 28566424 Free PMC article.