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Page 1
Discovery and optimization of aminopyrimidinones as potent and state-dependent Nav1.7 antagonists.
Nguyen HN, Bregman H, Buchanan JL, Du B, Feric E, Huang L, Li X, Ligutti J, Liu D, Malmberg AB, Matson DJ, McDermott JS, Patel VF, Wilenkin B, Zou A, McDonough SI, Dimauro EF. Nguyen HN, et al. Among authors: matson dj. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1055-60. doi: 10.1016/j.bmcl.2011.11.111. Epub 2011 Dec 6. Bioorg Med Chem Lett. 2012. PMID: 22209205
The discovery of benzoxazine sulfonamide inhibitors of NaV1.7: Tools that bridge efficacy and target engagement.
La DS, Peterson EA, Bode C, Boezio AA, Bregman H, Chu-Moyer MY, Coats J, DiMauro EF, Dineen TA, Du B, Gao H, Graceffa R, Gunaydin H, Guzman-Perez A, Fremeau R Jr, Huang X, Ilch C, Kornecook TJ, Kreiman C, Ligutti J, Jasmine Lin MH, McDermott JS, Marx I, Matson DJ, McDonough SI, Moyer BD, Nho Nguyen H, Taborn K, Yu V, Weiss MM. La DS, et al. Among authors: matson dj. Bioorg Med Chem Lett. 2017 Aug 1;27(15):3477-3485. doi: 10.1016/j.bmcl.2017.05.070. Epub 2017 Jun 1. Bioorg Med Chem Lett. 2017. PMID: 28629594
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
Bregman H, Berry L, Buchanan JL, Chen A, Du B, Feric E, Hierl M, Huang L, Immke D, Janosky B, Johnson D, Li X, Ligutti J, Liu D, Malmberg A, Matson D, McDermott J, Miu P, Nguyen HN, Patel VF, Waldon D, Wilenkin B, Zheng XM, Zou A, McDonough SI, DiMauro EF. Bregman H, et al. J Med Chem. 2011 Jul 14;54(13):4427-45. doi: 10.1021/jm200018k. Epub 2011 Jun 2. J Med Chem. 2011. PMID: 21634377
Inhibition of Inactive States of Tetrodotoxin-Sensitive Sodium Channels Reduces Spontaneous Firing of C-Fiber Nociceptors and Produces Analgesia in Formalin and Complete Freund's Adjuvant Models of Pain.
Matson DJ, Hamamoto DT, Bregman H, Cooke M, DiMauro EF, Huang L, Johnson D, Li X, McDermott J, Morgan C, Wilenkin B, Malmberg AB, McDonough SI, Simone DA. Matson DJ, et al. PLoS One. 2015 Sep 17;10(9):e0138140. doi: 10.1371/journal.pone.0138140. eCollection 2015. PLoS One. 2015. PMID: 26379236 Free PMC article.
Pharmacologic Characterization of AMG8379, a Potent and Selective Small Molecule Sulfonamide Antagonist of the Voltage-Gated Sodium Channel NaV1.7.
Kornecook TJ, Yin R, Altmann S, Be X, Berry V, Ilch CP, Jarosh M, Johnson D, Lee JH, Lehto SG, Ligutti J, Liu D, Luther J, Matson D, Ortuno D, Roberts J, Taborn K, Wang J, Weiss MM, Yu V, Zhu DXD, Fremeau RT Jr, Moyer BD. Kornecook TJ, et al. J Pharmacol Exp Ther. 2017 Jul;362(1):146-160. doi: 10.1124/jpet.116.239590. Epub 2017 May 4. J Pharmacol Exp Ther. 2017. PMID: 28473457
Pharmacological effects of nonselective and subtype-selective nicotinic acetylcholine receptor agonists in animal models of persistent pain.
Gao B, Hierl M, Clarkin K, Juan T, Nguyen H, van der Valk M, Deng H, Guo W, Lehto SG, Matson D, McDermott JS, Knop J, Gaida K, Cao L, Waldon D, Albrecht BK, Boezio AA, Copeland KW, Harmange JC, Springer SK, Malmberg AB, McDonough SI. Gao B, et al. Pain. 2010 Apr;149(1):33-49. doi: 10.1016/j.pain.2010.01.007. Epub 2010 Feb 18. Pain. 2010. PMID: 20167427
Crystal structures of human glycine receptor α3 bound to a novel class of analgesic potentiators.
Huang X, Shaffer PL, Ayube S, Bregman H, Chen H, Lehto SG, Luther JA, Matson DJ, McDonough SI, Michelsen K, Plant MH, Schneider S, Simard JR, Teffera Y, Yi S, Zhang M, DiMauro EF, Gingras J. Huang X, et al. Among authors: matson dj. Nat Struct Mol Biol. 2017 Feb;24(2):108-113. doi: 10.1038/nsmb.3329. Epub 2016 Dec 19. Nat Struct Mol Biol. 2017. PMID: 27991902
Rat NaV1.7 loss-of-function genetic model: Deficient nociceptive and neuropathic pain behavior with retained olfactory function and intra-epidermal nerve fibers.
Grubinska B, Chen L, Alsaloum M, Rampal N, Matson DJ, Yang C, Taborn K, Zhang M, Youngblood B, Liu D, Galbreath E, Allred S, Lepherd M, Ferrando R, Kornecook TJ, Lehto SG, Waxman SG, Moyer BD, Dib-Hajj S, Gingras J. Grubinska B, et al. Among authors: matson dj. Mol Pain. 2019 Jan-Dec;15:1744806919881846. doi: 10.1177/1744806919881846. Mol Pain. 2019. PMID: 31550995 Free PMC article.
Aminoquinazolines as TRPV1 antagonists: modulation of drug-like properties through the exploration of 2-position substitution.
Blum CA, Zheng X, Brielmann H, Hodgetts KJ, Bakthavatchalam R, Chandrasekhar J, Krause JE, Cortright D, Matson D, Crandall M, Ngo CK, Fung L, Day M, Kershaw M, De Lombaert S, Chenard BL. Blum CA, et al. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4573-7. doi: 10.1016/j.bmcl.2008.07.036. Epub 2008 Jul 15. Bioorg Med Chem Lett. 2008. PMID: 18662872
16 results