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Page 1
Integrative structural and functional analysis of human malic enzyme 3: A potential therapeutic target for pancreatic cancer.
Grell TAJ, Mason M, Thompson AA, Gómez-Tamayo JC, Riley D, Wagner MV, Steele R, Ortiz-Meoz RF, Wadia J, Shaffer PL, Tresadern G, Sharma S, Yu X. Grell TAJ, et al. Among authors: shaffer pl. Heliyon. 2022 Dec 19;8(12):e12392. doi: 10.1016/j.heliyon.2022.e12392. eCollection 2022 Dec. Heliyon. 2022. PMID: 36590518 Free PMC article.
Structure of human spermine oxidase in complex with a highly selective allosteric inhibitor.
Diaz E, Adhikary S, Tepper AWJW, Riley D, Ortiz-Meoz R, Krosky D, Buyck C, Lamenca CM, Llaveria J, Fang L, Kalin JH, Klaren VNA, Fahmy S, Shaffer PL, Kirkpatrick R, Carbajo RJ, Thomsen M, Impagliazzo A. Diaz E, et al. Among authors: shaffer pl. Commun Biol. 2022 Aug 5;5(1):787. doi: 10.1038/s42003-022-03735-9. Commun Biol. 2022. PMID: 35931745 Free PMC article.
Diazaspirononane Nonsaccharide Inhibitors of O-GlcNAcase (OGA) for the Treatment of Neurodegenerative Disorders.
Martínez-Viturro CM, Trabanco AA, Royes J, Fernández E, Tresadern G, Vega JA, Del Cerro A, Delgado F, García Molina A, Tovar F, Shaffer P, Ebneth A, Bretteville A, Mertens L, Somers M, Alonso JM, Bartolomé-Nebreda JM. Martínez-Viturro CM, et al. J Med Chem. 2020 Nov 25;63(22):14017-14044. doi: 10.1021/acs.jmedchem.0c01479. Epub 2020 Nov 16. J Med Chem. 2020. PMID: 33197187
Discovery of Potent and Orally Bioavailable Pyridine N-Oxide-Based Factor XIa Inhibitors through Exploiting Nonclassical Interactions.
Xu G, Liu Z, Wang X, Lu T, DesJarlais RL, Thieu T, Zhang J, Devine ZH, Du F, Li Q, Milligan CM, Shaffer P, Cedervall PE, Spurlino JC, Stratton CF, Pietrak B, Szewczuk LM, Wong V, Steele RA, Bruinzeel W, Chintala M, Silva J, Gaul MD, Macielag MJ, Nargund R. Xu G, et al. J Med Chem. 2022 Aug 11;65(15):10419-10440. doi: 10.1021/acs.jmedchem.2c00442. Epub 2022 Jul 21. J Med Chem. 2022. PMID: 35862732
Diazepinone HBV capsid assembly modulators.
Kuduk SD, DeRatt LG, Stoops B, Shaffer P, Lam AM, Espiritu C, Vogel R, Lau V, Flores OA, Hartman GD. Kuduk SD, et al. Bioorg Med Chem Lett. 2022 Sep 15;72:128823. doi: 10.1016/j.bmcl.2022.128823. Epub 2022 May 27. Bioorg Med Chem Lett. 2022. PMID: 35644301
A carboxylic acid isostere screen of the DHODH inhibitor Brequinar.
DeRatt LG, Christine Pietsch E, Tanner A, Shaffer P, Jacoby E, Wang W, Kazmi F, Zhang X, Attar RM, Edwards JP, Kuduk SD. DeRatt LG, et al. Bioorg Med Chem Lett. 2020 Nov 15;30(22):127589. doi: 10.1016/j.bmcl.2020.127589. Epub 2020 Sep 29. Bioorg Med Chem Lett. 2020. PMID: 33007394
Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction.
Gonzalez AZ, Eksterowicz J, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Duquette J, Fox BM, Fu J, Huang X, Houze JB, Jin L, Li Y, Li Z, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, McMinn DL, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Medina JC, Sun D. Gonzalez AZ, et al. J Med Chem. 2014 Mar 27;57(6):2472-88. doi: 10.1021/jm401767k. Epub 2014 Mar 4. J Med Chem. 2014. PMID: 24548297
Modulation of Ligand-Gated Glycine Receptors Via Functional Monoclonal Antibodies.
Simard JR, Michelsen K, Wang Y, Yang C, Youngblood B, Grubinska B, Taborn K, Gillie DJ, Cook K, Chung K, Long AM, Hall BE, Shaffer PL, Foti RS, Gingras J. Simard JR, et al. Among authors: shaffer pl. J Pharmacol Exp Ther. 2022 Oct;383(1):56-69. doi: 10.1124/jpet.121.001026. Epub 2022 Aug 4. J Pharmacol Exp Ther. 2022. PMID: 35926871
Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.
Sun D, Li Z, Rew Y, Gribble M, Bartberger MD, Beck HP, Canon J, Chen A, Chen X, Chow D, Deignan J, Duquette J, Eksterowicz J, Fisher B, Fox BM, Fu J, Gonzalez AZ, Gonzalez-Lopez De Turiso F, Houze JB, Huang X, Jiang M, Jin L, Kayser F, Liu JJ, Lo MC, Long AM, Lucas B, McGee LR, McIntosh J, Mihalic J, Oliner JD, Osgood T, Peterson ML, Roveto P, Saiki AY, Shaffer P, Toteva M, Wang Y, Wang YC, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Yu M, Zhao X, Zhou J, Zhu J, Olson SH, Medina JC. Sun D, et al. J Med Chem. 2014 Feb 27;57(4):1454-72. doi: 10.1021/jm401753e. Epub 2014 Feb 5. J Med Chem. 2014. PMID: 24456472
28 results