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Page 1
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.
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.
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
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
Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.
Peterson EA, Boezio AA, Andrews PS, Boezio CM, Bush TL, Cheng AC, Choquette D, Coats JR, Colletti AE, Copeland KW, DuPont M, Graceffa R, Grubinska B, Kim JL, Lewis RT, Liu J, Mullady EL, Potashman MH, Romero K, Shaffer PL, Stanton MK, Stellwagen JC, Teffera Y, Yi S, Cai T, La DS. Peterson EA, et al. Among authors: shaffer pl. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4967-74. doi: 10.1016/j.bmcl.2012.06.033. Epub 2012 Jun 16. Bioorg Med Chem Lett. 2012. PMID: 22765895
Rational design and binding mode duality of MDM2-p53 inhibitors.
Gonzalez-Lopez de Turiso F, Sun D, Rew Y, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Correll TL, Huang X, Julian LD, Kayser F, Lo MC, Long AM, McMinn D, Oliner JD, Osgood T, Powers JP, Saiki AY, Schneider S, Shaffer P, Xiao SH, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Medina JC, Olson SH. Gonzalez-Lopez de Turiso F, et al. J Med Chem. 2013 May 23;56(10):4053-70. doi: 10.1021/jm400293z. Epub 2013 May 6. J Med Chem. 2013. PMID: 23597064
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
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
30 results