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Page 1
Discovery of pyridyl urea sulfonamide inhibitors of NaV1.7.
Butler JR, Rescourio G, Milgram BC, Foti RS, Kornecook T, Ligutti J, Moyer BD, Taborn K, Youngblood BD, Yu V, Shimanovich R, Boezio A, Weiss M. Butler JR, et al. Among authors: kornecook t. Bioorg Med Chem Lett. 2022 Oct 1;73:128892. doi: 10.1016/j.bmcl.2022.128892. Epub 2022 Jul 16. Bioorg Med Chem Lett. 2022. PMID: 35850422
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
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: kornecook tj. 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
Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors.
DiMauro EF, Altmann S, Berry LM, Bregman H, Chakka N, Chu-Moyer M, Bojic EF, Foti RS, Fremeau R, Gao H, Gunaydin H, Guzman-Perez A, Hall BE, Huang H, Jarosh M, Kornecook T, Lee J, Ligutti J, Liu D, Moyer BD, Ortuno D, Rose PE, Schenkel LB, Taborn K, Wang J, Wang Y, Yu V, Weiss MM. DiMauro EF, et al. Among authors: kornecook t. J Med Chem. 2016 Sep 8;59(17):7818-39. doi: 10.1021/acs.jmedchem.6b00425. Epub 2016 Aug 29. J Med Chem. 2016. PMID: 27441383
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement.
Marx IE, Dineen TA, Able J, Bode C, Bregman H, Chu-Moyer M, DiMauro EF, Du B, Foti RS, Fremeau RT Jr, Gao H, Gunaydin H, Hall BE, Huang L, Kornecook T, Kreiman CR, La DS, Ligutti J, Lin MJ, Liu D, McDermott JS, Moyer BD, Peterson EA, Roberts JT, Rose P, Wang J, Youngblood BD, Yu V, Weiss MM. Marx IE, et al. Among authors: kornecook t. ACS Med Chem Lett. 2016 Sep 21;7(12):1062-1067. doi: 10.1021/acsmedchemlett.6b00243. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994738 Free PMC article.
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities.
Weiss MM, Dineen TA, Marx IE, Altmann S, Boezio A, Bregman H, Chu-Moyer M, DiMauro EF, Feric Bojic E, Foti RS, Gao H, Graceffa R, Gunaydin H, Guzman-Perez A, Huang H, Huang L, Jarosh M, Kornecook T, Kreiman CR, Ligutti J, La DS, Lin MJ, Liu D, Moyer BD, Nguyen HN, Peterson EA, Rose PE, Taborn K, Youngblood BD, Yu V, Fremeau RT Jr. Weiss MM, et al. Among authors: kornecook t. J Med Chem. 2017 Jul 27;60(14):5969-5989. doi: 10.1021/acs.jmedchem.6b01851. Epub 2017 Apr 20. J Med Chem. 2017. PMID: 28287723
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity.
Graceffa RF, Boezio AA, Able J, Altmann S, Berry LM, Boezio C, Butler JR, Chu-Moyer M, Cooke M, DiMauro EF, Dineen TA, Feric Bojic E, Foti RS, Fremeau RT Jr, Guzman-Perez A, Gao H, Gunaydin H, Huang H, Huang L, Ilch C, Jarosh M, Kornecook T, Kreiman CR, La DS, Ligutti J, Milgram BC, Lin MJ, Marx IE, Nguyen HN, Peterson EA, Rescourio G, Roberts J, Schenkel L, Shimanovich R, Sparling BA, Stellwagen J, Taborn K, Vaida KR, Wang J, Yeoman J, Yu V, Zhu D, Moyer BD, Weiss MM. Graceffa RF, et al. Among authors: kornecook t. J Med Chem. 2017 Jul 27;60(14):5990-6017. doi: 10.1021/acs.jmedchem.6b01850. Epub 2017 Apr 20. J Med Chem. 2017. PMID: 28324649
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: kornecook tj. Mol Pain. 2019 Jan-Dec;15:1744806919881846. doi: 10.1177/1744806919881846. Mol Pain. 2019. PMID: 31550995 Free PMC article.
Discovery and hit-to-lead evaluation of piperazine amides as selective, state-dependent NaV1.7 inhibitors.
Sparling BA, Yi S, Able J, Bregman H, DiMauro EF, Foti RS, Gao H, Guzman-Perez A, Huang H, Jarosh M, Kornecook T, Ligutti J, Milgram BC, Moyer BD, Youngblood B, Yu VL, Weiss MM. Sparling BA, et al. Among authors: kornecook t. Medchemcomm. 2016 Dec 2;8(4):744-754. doi: 10.1039/c6md00578k. eCollection 2017 Apr 1. Medchemcomm. 2016. PMID: 30108793 Free PMC article.
Discovery of Tarantula Venom-Derived NaV1.7-Inhibitory JzTx-V Peptide 5-Br-Trp24 Analogue AM-6120 with Systemic Block of Histamine-Induced Pruritis.
Wu B, Murray JK, Andrews KL, Sham K, Long J, Aral J, Ligutti J, Amagasu S, Liu D, Zou A, Min X, Wang Z, Ilch CP, Kornecook TJ, Lin MJ, Be X, Miranda LP, Moyer BD, Biswas K. Wu B, et al. Among authors: kornecook tj. J Med Chem. 2018 Nov 8;61(21):9500-9512. doi: 10.1021/acs.jmedchem.8b00736. Epub 2018 Oct 22. J Med Chem. 2018. PMID: 30346167
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