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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: reel jk. 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
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. Nat Med. 2016 Dec;22(12):1496-1501. doi: 10.1038/nm.4221. Epub 2016 Nov 7. Nat Med. 2016. PMID: 27820603
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. 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
Electroencephalographic, cognitive, and neurochemical effects of LY3130481 (CERC-611), a selective antagonist of TARP-γ8-associated AMPA receptors.
Witkin JM, Li J, Gilmour G, Mitchell SN, Carter G, Gleason SD, Seidel WF, Eastwood BJ, McCarthy A, Porter WJ, Reel J, Gardinier KM, Kato AS, Wafford KA. Witkin JM, et al. Neuropharmacology. 2017 Nov;126:257-270. doi: 10.1016/j.neuropharm.2017.07.028. Epub 2017 Jul 28. Neuropharmacology. 2017. PMID: 28757050
Discovery and SAR studies of novel GlyT1 inhibitors.
Walter MW, Hoffman BJ, Gordon K, Johnson K, Love P, Jones M, Man T, Phebus L, Reel JK, Rudyk HC, Shannon H, Svensson K, Yu H, Valli MJ, Porter WJ. Walter MW, et al. Among authors: reel jk. Bioorg Med Chem Lett. 2007 Sep 15;17(18):5233-8. doi: 10.1016/j.bmcl.2007.06.074. Epub 2007 Jun 30. Bioorg Med Chem Lett. 2007. PMID: 17629697
Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.
Engler TA, Henry JR, Malhotra S, Cunningham B, Furness K, Brozinick J, Burkholder TP, Clay MP, Clayton J, Diefenbacher C, Hawkins E, Iversen PW, Li Y, Lindstrom TD, Marquart AL, McLean J, Mendel D, Misener E, Briere D, O'Toole JC, Porter WJ, Queener S, Reel JK, Owens RA, Brier RA, Eessalu TE, Wagner JR, Campbell RM, Vaughn R. Engler TA, et al. Among authors: reel jk. J Med Chem. 2004 Jul 29;47(16):3934-7. doi: 10.1021/jm049768a. J Med Chem. 2004. PMID: 15267232
The development of potent and selective bisarylmaleimide GSK3 inhibitors.
Engler TA, Malhotra S, Burkholder TP, Henry JR, Mendel D, Porter WJ, Furness K, Diefenbacher C, Marquart A, Reel JK, Li Y, Clayton J, Cunningham B, McLean J, O'toole JC, Brozinick J, Hawkins E, Misener E, Briere D, Brier RA, Wagner JR, Campbell RM, Anderson BD, Vaughn R, Bennett DB, Meier TI, Cook JA. Engler TA, et al. Among authors: reel jk. Bioorg Med Chem Lett. 2005 Feb 15;15(4):899-903. doi: 10.1016/j.bmcl.2004.12.063. Bioorg Med Chem Lett. 2005. PMID: 15686883
16 results