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Page 1
Electrophilic properties of itaconate and derivatives regulate the IκBζ-ATF3 inflammatory axis.
Bambouskova M, Gorvel L, Lampropoulou V, Sergushichev A, Loginicheva E, Johnson K, Korenfeld D, Mathyer ME, Kim H, Huang LH, Duncan D, Bregman H, Keskin A, Santeford A, Apte RS, Sehgal R, Johnson B, Amarasinghe GK, Soares MP, Satoh T, Akira S, Hai T, de Guzman Strong C, Auclair K, Roddy TP, Biller SA, Jovanovic M, Klechevsky E, Stewart KM, Randolph GJ, Artyomov MN. Bambouskova M, et al. Among authors: bregman h. Nature. 2018 Apr;556(7702):501-504. doi: 10.1038/s41586-018-0052-z. Epub 2018 Apr 18. Nature. 2018. PMID: 29670287 Free PMC article.
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: bregman h. 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
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: bregman h. 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.
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: bregman h. 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
The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors.
Bregman H, Simard JR, Andrews KL, Ayube S, Chen H, Gunaydin H, Guzman-Perez A, Hu J, Huang L, Huang X, Krolikowski PH, Lehto SG, Lewis RT, Michelsen K, Pegman P, Plant MH, Shaffer PL, Teffera Y, Yi S, Zhang M, Gingras J, DiMauro EF. Bregman H, et al. J Med Chem. 2017 Feb 9;60(3):1105-1125. doi: 10.1021/acs.jmedchem.6b01496. Epub 2016 Dec 21. J Med Chem. 2017. PMID: 28001399
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: bregman h. 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.
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: bregman h. 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
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: bregman h. Medchemcomm. 2016 Dec 2;8(4):744-754. doi: 10.1039/c6md00578k. eCollection 2017 Apr 1. Medchemcomm. 2016. PMID: 30108793 Free PMC article.
52 results