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Page 1
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: porter wj. 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
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: porter wj. J Med Chem. 2004 Jul 29;47(16):3934-7. doi: 10.1021/jm049768a. J Med Chem. 2004. PMID: 15267232
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: porter wj. 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
Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.
Winneroski LL, Erickson JA, Green SJ, Lopez JE, Stout SL, Porter WJ, Timm DE, Audia JE, Barberis M, Beck JP, Boggs LN, Borders AR, Boyer RD, Brier RA, Hembre EJ, Hendle J, Garcia-Losada P, Minguez JM, Mathes BM, May PC, Monk SA, Rankovic Z, Shi Y, Watson BM, Yang Z, Mergott DJ. Winneroski LL, et al. Among authors: porter wj. Bioorg Med Chem. 2020 Jan 1;28(1):115194. doi: 10.1016/j.bmc.2019.115194. Epub 2019 Nov 15. Bioorg Med Chem. 2020. PMID: 31786008
Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor.
McKinzie DL, Winneroski LL, Green SJ, Hembre EJ, Erickson JA, Willis BA, Monk SA, Aluise CD, Baker TK, Lopez JE, Hendle J, Beck JP, Brier RA, Boggs LN, Borders AR, Cocke PJ, Garcia-Losada P, Lowe SL, Mathes BM, May PC, Porter WJ, Stout SL, Timm DE, Watson BM, Yang Z, Mergott DJ. McKinzie DL, et al. Among authors: porter wj. J Med Chem. 2021 Jun 24;64(12):8076-8100. doi: 10.1021/acs.jmedchem.1c00489. Epub 2021 Jun 3. J Med Chem. 2021. PMID: 34081466
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: porter wj. 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
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: porter wj. CNS Neurol Disord Drug Targets. 2017;16(10):1099-1110. doi: 10.2174/1871527316666171101132047. CNS Neurol Disord Drug Targets. 2017. PMID: 29090671
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. Among authors: porter wj. Neuropharmacology. 2017 Nov;126:257-270. doi: 10.1016/j.neuropharm.2017.07.028. Epub 2017 Jul 28. Neuropharmacology. 2017. PMID: 28757050
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
30 results