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389 results

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Page 1
Implementation of the CYP Index for the Design of Selective Tryptophan-2,3-dioxygenase Inhibitors.
Parr BT, Pastor R, Sellers BD, Pei Z, Jaipuri FA, Castanedo GM, Gazzard L, Kumar S, Li X, Liu W, Mendonca R, Pavana RK, Potturi H, Shao C, Velvadapu V, Waldo JP, Wu G, Yuen PW, Zhang Z, Zhang Y, Harris SF, Oh AJ, DiPasquale A, Dement K, La H, Goon L, Gustafson A, VanderPorten EC, Mautino MR, Liu Y. Parr BT, et al. Among authors: gustafson a. ACS Med Chem Lett. 2020 Mar 4;11(4):541-549. doi: 10.1021/acsmedchemlett.0c00004. eCollection 2020 Apr 9. ACS Med Chem Lett. 2020. PMID: 32292562 Free PMC article.
Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models.
Patel S, Cohen F, Dean BJ, De La Torre K, Deshmukh G, Estrada AA, Ghosh AS, Gibbons P, Gustafson A, Huestis MP, Le Pichon CE, Lin H, Liu W, Liu X, Liu Y, Ly CQ, Lyssikatos JP, Ma C, Scearce-Levie K, Shin YG, Solanoy H, Stark KL, Wang J, Wang B, Zhao X, Lewcock JW, Siu M. Patel S, et al. Among authors: gustafson a. J Med Chem. 2015 Jan 8;58(1):401-18. doi: 10.1021/jm5013984. Epub 2014 Oct 23. J Med Chem. 2015. PMID: 25341110
Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).
Patel S, Harris SF, Gibbons P, Deshmukh G, Gustafson A, Kellar T, Lin H, Liu X, Liu Y, Liu Y, Ma C, Scearce-Levie K, Ghosh AS, Shin YG, Solanoy H, Wang J, Wang B, Yin J, Siu M, Lewcock JW. Patel S, et al. Among authors: gustafson a. J Med Chem. 2015 Oct 22;58(20):8182-99. doi: 10.1021/acs.jmedchem.5b01072. Epub 2015 Oct 2. J Med Chem. 2015. PMID: 26431428
Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design.
Volgraf M, Sellers BD, Jiang Y, Wu G, Ly CQ, Villemure E, Pastor RM, Yuen PW, Lu A, Luo X, Liu M, Zhang S, Sun L, Fu Y, Lupardus PJ, Wallweber HJ, Liederer BM, Deshmukh G, Plise E, Tay S, Reynen P, Herrington J, Gustafson A, Liu Y, Dirksen A, Dietz MG, Liu Y, Wang TM, Hanson JE, Hackos D, Scearce-Levie K, Schwarz JB. Volgraf M, et al. Among authors: gustafson a. J Med Chem. 2016 Mar 24;59(6):2760-79. doi: 10.1021/acs.jmedchem.5b02010. Epub 2016 Mar 8. J Med Chem. 2016. PMID: 26919761
Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies.
Liang J, Zhang B, Labadie S, Ortwine DF, Vinogradova M, Kiefer JR, Gehling VS, Harmange JC, Cummings R, Lai T, Liao J, Zheng X, Liu Y, Gustafson A, Van der Porten E, Mao W, Liederer BM, Deshmukh G, Classon M, Trojer P, Dragovich PS, Murray L. Liang J, et al. Among authors: gustafson a. Bioorg Med Chem Lett. 2016 Aug 15;26(16):4036-41. doi: 10.1016/j.bmcl.2016.06.078. Epub 2016 Jun 29. Bioorg Med Chem Lett. 2016. PMID: 27406798
Identification of potent, selective KDM5 inhibitors.
Gehling VS, Bellon SF, Harmange JC, LeBlanc Y, Poy F, Odate S, Buker S, Lan F, Arora S, Williamson KE, Sandy P, Cummings RT, Bailey CM, Bergeron L, Mao W, Gustafson A, Liu Y, VanderPorten E, Audia JE, Trojer P, Albrecht BK. Gehling VS, et al. Among authors: gustafson a. Bioorg Med Chem Lett. 2016 Sep 1;26(17):4350-4. doi: 10.1016/j.bmcl.2016.07.026. Epub 2016 Jul 19. Bioorg Med Chem Lett. 2016. PMID: 27476424
Design and evaluation of 1,7-naphthyridones as novel KDM5 inhibitors.
Labadie SS, Dragovich PS, Cummings RT, Deshmukh G, Gustafson A, Han N, Harmange JC, Kiefer JR, Li Y, Liang J, Liederer BM, Liu Y, Manieri W, Mao W, Murray L, Ortwine DF, Trojer P, VanderPorten E, Vinogradova M, Wen L. Labadie SS, et al. Among authors: gustafson a. Bioorg Med Chem Lett. 2016 Sep 15;26(18):4492-4496. doi: 10.1016/j.bmcl.2016.07.070. Epub 2016 Jul 29. Bioorg Med Chem Lett. 2016. PMID: 27499454
A novel NMDA receptor positive allosteric modulator that acts via the transmembrane domain.
Wang TM, Brown BM, Deng L, Sellers BD, Lupardus PJ, Wallweber HJA, Gustafson A, Wong E, Volgraf M, Schwarz JB, Hackos DH, Hanson JE. Wang TM, et al. Among authors: gustafson a. Neuropharmacology. 2017 Jul 15;121:204-218. doi: 10.1016/j.neuropharm.2017.04.041. Epub 2017 Apr 27. Neuropharmacology. 2017. PMID: 28457974 Free article.
From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.
Liang J, Labadie S, Zhang B, Ortwine DF, Patel S, Vinogradova M, Kiefer JR, Mauer T, Gehling VS, Harmange JC, Cummings R, Lai T, Liao J, Zheng X, Liu Y, Gustafson A, Van der Porten E, Mao W, Liederer BM, Deshmukh G, An L, Ran Y, Classon M, Trojer P, Dragovich PS, Murray L. Liang J, et al. Among authors: gustafson a. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2974-2981. doi: 10.1016/j.bmcl.2017.05.016. Epub 2017 May 5. Bioorg Med Chem Lett. 2017. PMID: 28512031
Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease.
Patel S, Meilandt WJ, Erickson RI, Chen J, Deshmukh G, Estrada AA, Fuji RN, Gibbons P, Gustafson A, Harris SF, Imperio J, Liu W, Liu X, Liu Y, Lyssikatos JP, Ma C, Yin J, Lewcock JW, Siu M. Patel S, et al. Among authors: gustafson a. J Med Chem. 2017 Oct 12;60(19):8083-8102. doi: 10.1021/acs.jmedchem.7b00843. Epub 2017 Sep 20. J Med Chem. 2017. PMID: 28929759
389 results