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Page 1
Engineering NaV1.7 Inhibitory JzTx-V Peptides with a Potency and Basicity Profile Suitable for Antibody Conjugation To Enhance Pharmacokinetics.
Murray JK, Wu B, Tegley CM, Nixey TE, Falsey JR, Herberich B, Yin L, Sham K, Long J, Aral J, Cheng Y, Netirojjanakul C, Doherty L, Glaus C, Ikotun T, Li H, Tran L, Soto M, Salimi-Moosavi H, Ligutti J, Amagasu S, Andrews KL, Be X, Lin MJ, Foti RS, Ilch CP, Youngblood B, Kornecook TJ, Karow M, Walker KW, Moyer BD, Biswas K, Miranda LP. Murray JK, et al. Among authors: youngblood b. ACS Chem Biol. 2019 Apr 19;14(4):806-818. doi: 10.1021/acschembio.9b00183. Epub 2019 Mar 27. ACS Chem Biol. 2019. PMID: 30875193
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. 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
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. 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
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: youngblood bd. 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.
Correction to "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, Nguyen HN, Peterson EA, Roberts JT, Rose P, Wang J, Youngblood BD, Yu V, Weiss MM. Marx IE, et al. Among authors: youngblood bd. ACS Med Chem Lett. 2017 Feb 28;8(3):378. doi: 10.1021/acsmedchemlett.7b00075. eCollection 2017 Mar 9. ACS Med Chem Lett. 2017. PMID: 28337335 Free PMC article.
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: youngblood b. 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: youngblood b. Medchemcomm. 2016 Dec 2;8(4):744-754. doi: 10.1039/c6md00578k. eCollection 2017 Apr 1. Medchemcomm. 2016. PMID: 30108793 Free PMC article.
Modulation of Ligand-Gated Glycine Receptors Via Functional Monoclonal Antibodies.
Simard JR, Michelsen K, Wang Y, Yang C, Youngblood B, Grubinska B, Taborn K, Gillie DJ, Cook K, Chung K, Long AM, Hall BE, Shaffer PL, Foti RS, Gingras J. Simard JR, et al. Among authors: youngblood b. J Pharmacol Exp Ther. 2022 Oct;383(1):56-69. doi: 10.1124/jpet.121.001026. Epub 2022 Aug 4. J Pharmacol Exp Ther. 2022. PMID: 35926871
AMG2850, a potent and selective TRPM8 antagonist, is not effective in rat models of inflammatory mechanical hypersensitivity and neuropathic tactile allodynia.
Lehto SG, Weyer AD, Zhang M, Youngblood BD, Wang J, Wang W, Kerstein PC, Davis C, Wild KD, Stucky CL, Gavva NR. Lehto SG, et al. Naunyn Schmiedebergs Arch Pharmacol. 2015 Apr;388(4):465-76. doi: 10.1007/s00210-015-1090-9. Epub 2015 Feb 10. Naunyn Schmiedebergs Arch Pharmacol. 2015. PMID: 25662185 Free PMC article.
156 results