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Items: 12

1.

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.

J Pharmacol Exp Ther. 2019 Jun;369(3):345-363. doi: 10.1124/jpet.118.250126. Epub 2019 Mar 25.

PMID:
30910921
2.

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.

CNS Neurol Disord Drug Targets. 2017;16(10):1099-1110. doi: 10.2174/1871527316666171101132047.

PMID:
29090671
3.

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.

ACS Chem Neurosci. 2017 Dec 20;8(12):2631-2647. doi: 10.1021/acschemneuro.7b00186. Epub 2017 Sep 5.

PMID:
28825787
4.

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.

Nat Med. 2016 Dec;22(12):1496-1501. doi: 10.1038/nm.4221. Epub 2016 Nov 7.

PMID:
27820603
5.

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.

J Med Chem. 2016 May 26;59(10):4753-68. doi: 10.1021/acs.jmedchem.6b00125. Epub 2016 Apr 29.

PMID:
27067148
6.

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.

J Pharmacol Exp Ther. 2014 Oct;351(1):124-33. doi: 10.1124/jpet.114.212779. Epub 2014 Jul 15.

PMID:
25027316
7.

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.

ACS Med Chem Lett. 2013 May 7;4(6):560-4. doi: 10.1021/ml400049p. eCollection 2013 Jun 13.

8.

Transmembrane AMPA receptor regulatory proteins and cornichon-2 allosterically regulate AMPA receptor antagonists and potentiators.

Schober DA, Gill MB, Yu H, Gernert DL, Jeffries MW, Ornstein PL, Kato AS, Felder CC, Bredt DS.

J Biol Chem. 2011 Apr 15;286(15):13134-42. doi: 10.1074/jbc.M110.212522. Epub 2011 Feb 22.

9.

(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.

J Med Chem. 2007 Dec 27;50(26):6443-5. Epub 2007 Nov 27.

PMID:
18038968
10.

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.

Bioorg Med Chem Lett. 2004 Jun 7;14(11):2759-63.

PMID:
15125928
11.

Design and synthesis of fluorinated RXR modulators.

Gernert DL, Ajamie R, Ardecky RA, Bell MG, Leibowitz MD, Mais DA, Mapes CM, Michellys PY, Rungta D, Reifel-Miller A, Tyhonas JS, Yumibe N, Grese TA.

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3191-5.

PMID:
12951091
12.

In vitro studies of a bradykinin B1/B2 antagonist linked to a human neutrophil elastase inhibitor; a heterodimer for the treatment of inflammatory disorders.

Leimer AH, Kroona HB, Blodgett JK, Whalley ET, Ross SE, Burkard MR, Zuzack JS, Gernert DL, Dyckes DF.

Can J Physiol Pharmacol. 1997 Jun;75(6):633-8.

PMID:
9276141

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