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Page 1
Forebrain-selective AMPA-receptor antagonism guided by TARP γ-8 as an antiepileptic mechanism.
Kato AS, Burris KD, Gardinier KM, Gernert DL, Porter WJ, Reel J, Ding C, Tu Y, Schober DA, Lee MR, Heinz BA, Fitch TE, Gleason SD, Catlow JT, Yu H, Fitzjohn SM, Pasqui F, Wang H, Qian Y, Sher E, Zwart R, Wafford KA, Rasmussen K, Ornstein PL, Isaac JT, Nisenbaum ES, Bredt DS, Witkin JM. Kato AS, et al. Among authors: gernert dl. Nat Med. 2016 Dec;22(12):1496-1501. doi: 10.1038/nm.4221. Epub 2016 Nov 7. Nat Med. 2016. PMID: 27820603
Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8.
Gardinier KM, Gernert DL, Porter WJ, Reel JK, Ornstein PL, Spinazze P, Stevens FC, Hahn P, Hollinshead SP, Mayhugh D, Schkeryantz J, Khilevich A, De Frutos O, Gleason SD, Kato AS, Luffer-Atlas D, Desai PV, Swanson S, Burris KD, Ding C, Heinz BA, Need AB, Barth VN, Stephenson GA, Diseroad BA, Woods TA, Yu H, Bredt D, Witkin JM. Gardinier KM, et al. Among authors: gernert dl. J Med Chem. 2016 May 26;59(10):4753-68. doi: 10.1021/acs.jmedchem.6b00125. Epub 2016 Apr 29. J Med Chem. 2016. PMID: 27067148
Structural Determinants of the γ-8 TARP Dependent AMPA Receptor Antagonist.
Lee MR, Gardinier KM, Gernert DL, Schober DA, Wright RA, Wang H, Qian Y, Witkin JM, Nisenbaum ES, Kato AS. Lee MR, et al. Among authors: gernert dl. ACS Chem Neurosci. 2017 Dec 20;8(12):2631-2647. doi: 10.1021/acschemneuro.7b00186. Epub 2017 Sep 5. ACS Chem Neurosci. 2017. PMID: 28825787
Targeted Blockade of TARP-γ8-Associated AMPA Receptors: Anticonvulsant Activity with the Selective Antagonist LY3130481 (CERC-611).
Witkin JM, Schober DA, Gleason SD, Catlow JT, Porter WJ, Reel J, Jin X, Hobbs J, Gehlert D, Gernert DL, Gardinier KM, Kato AS, Ping X, Smith JL. Witkin JM, et al. Among authors: gernert dl. CNS Neurol Disord Drug Targets. 2017;16(10):1099-1110. doi: 10.2174/1871527316666171101132047. CNS Neurol Disord Drug Targets. 2017. PMID: 29090671
Modulation of TARP γ8-Containing AMPA Receptors as a Novel Therapeutic Approach for Chronic Pain.
Knopp KL, Simmons RMA, Guo W, Adams BL, Gardinier KM, Gernert DL, Ornstein PL, Porter W, Reel J, Ding C, Wang H, Qian Y, Burris KD, Need A, Barth V, Swanson S, Catlow J, Witkin JM, Zwart R, Sher E, Choong KC, Wall TM, Schober D, Felder CC, Kato AS, Bredt DS, Nisenbaum ES. Knopp KL, et al. Among authors: gernert dl. J Pharmacol Exp Ther. 2019 Jun;369(3):345-363. doi: 10.1124/jpet.118.250126. Epub 2019 Mar 25. J Pharmacol Exp Ther. 2019. PMID: 30910921
Perampanel, an antagonist of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors, for the treatment of epilepsy: studies in human epileptic brain and nonepileptic brain and in rodent models.
Zwart R, Sher E, Ping X, Jin X, Sims JR Jr, Chappell AS, Gleason SD, Hahn PJ, Gardinier K, Gernert DL, Hobbs J, Smith JL, Valli SN, Witkin JM. Zwart R, et al. Among authors: gernert dl. J Pharmacol Exp Ther. 2014 Oct;351(1):124-33. doi: 10.1124/jpet.114.212779. Epub 2014 Jul 15. J Pharmacol Exp Ther. 2014. PMID: 25027316
Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor.
Dreyfus N, Myers JK, Badescu VO, de Frutos O, de la Puente ML, Ding C, Filla SA, Fynboe K, Gernert DL, Heinz BA, Hemrick-Luecke SK, Johnson KW, Johnson MP, López P, Love PL, Martin LJ, Masquelin T, McCoy MJ, Mendiola J, Morrow D, Muhlhauser M, Pascual G, Perun TJ, Pfeifer LA, Phebus LA, Richards SJ, Rincón JA, Seest EP, Shah J, Shaojuan J, Simmons RM, Stephenson GA, Tromiczak EG, Thompson LK, Walter MW, Weber WW, Zarrinmayeh H, Thomas CE, Joshi E, Iyengar S, Johansson AM. Dreyfus N, et al. Among authors: gernert dl. ACS Med Chem Lett. 2013 May 7;4(6):560-4. doi: 10.1021/ml400049p. eCollection 2013 Jun 13. ACS Med Chem Lett. 2013. PMID: 24900709 Free PMC article.
(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.
Bell MG, Gernert DL, Grese TA, Belvo MD, Borromeo PS, Kelley SA, Kennedy JH, Kolis SP, Lander PA, Richey R, Sharp VS, Stephenson GA, Williams JD, Yu H, Zimmerman KM, Steinberg MI, Jadhav PK. Bell MG, et al. Among authors: gernert dl. J Med Chem. 2007 Dec 27;50(26):6443-5. doi: 10.1021/jm701186z. Epub 2007 Nov 27. J Med Chem. 2007. PMID: 18038968
Design and synthesis of benzofused heterocyclic RXR modulators.
Gernert DL, Neel DA, Boehm MF, Leibowitz MD, Mais DA, Michellys PY, Rungta D, Reifel-Miller A, Grese TA. Gernert DL, et al. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2759-63. doi: 10.1016/j.bmcl.2004.03.073. Bioorg Med Chem Lett. 2004. PMID: 15125928
13 results