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The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells.
Fanning SW, Jeselsohn R, Dharmarajan V, Mayne CG, Karimi M, Buchwalter G, Houtman R, Toy W, Fowler CE, Han R, Lainé M, Carlson KE, Martin TA, Nowak J, Nwachukwu JC, Hosfield DJ, Chandarlapaty S, Tajkhorshid E, Nettles KW, Griffin PR, Shen Y, Katzenellenbogen JA, Brown M, Greene GL. Fanning SW, et al. Among authors: hosfield dj. Elife. 2018 Nov 29;7:e37161. doi: 10.7554/eLife.37161. Elife. 2018. PMID: 30489256 Free PMC article.
Discovery of a Glucocorticoid Receptor (GR) Activity Signature Using Selective GR Antagonism in ER-Negative Breast Cancer.
West DC, Kocherginsky M, Tonsing-Carter EY, Dolcen DN, Hosfield DJ, Lastra RR, Sinnwell JP, Thompson KJ, Bowie KR, Harkless RV, Skor MN, Pierce CF, Styke SC, Kim CR, de Wet L, Greene GL, Boughey JC, Goetz MP, Kalari KR, Wang L, Fleming GF, Györffy B, Conzen SD. West DC, et al. Among authors: hosfield dj. Clin Cancer Res. 2018 Jul 15;24(14):3433-3446. doi: 10.1158/1078-0432.CCR-17-2793. Epub 2018 Apr 10. Clin Cancer Res. 2018. PMID: 29636357 Free PMC article.
Structure-based design and discovery of potent and selective KDM5 inhibitors.
Nie Z, Shi L, Lai C, O'Connell SM, Xu J, Stansfield RK, Hosfield DJ, Veal JM, Stafford JA. Nie Z, et al. Among authors: hosfield dj. Bioorg Med Chem Lett. 2018 May 15;28(9):1490-1494. doi: 10.1016/j.bmcl.2018.03.083. Epub 2018 Mar 30. Bioorg Med Chem Lett. 2018. PMID: 29627262
Design, synthesis and biological evaluation of novel 4-phenylisoquinolinone BET bromodomain inhibitors.
Bennett MJ, Wu Y, Boloor A, Matuszkiewicz J, O'Connell SM, Shi L, Stansfield RK, Del Rosario JR, Veal JM, Hosfield DJ, Xu J, Kaldor SW, Stafford JA, Betancort JM. Bennett MJ, et al. Among authors: hosfield dj. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1811-1816. doi: 10.1016/j.bmcl.2018.04.016. Epub 2018 Apr 10. Bioorg Med Chem Lett. 2018. PMID: 29657099
Structure-based design and SAR development of 5,6-dihydroimidazolo[1,5-f]pteridine derivatives as novel Polo-like kinase-1 inhibitors.
Kiryanov A, Natala S, Jones B, McBride C, Feher V, Lam B, Liu Y, Honda K, Uchiyama N, Kawamoto T, Hikichi Y, Zhang L, Hosfield D, Skene R, Zou H, Stafford J, Cao X, Ichikawa T. Kiryanov A, et al. Bioorg Med Chem Lett. 2017 Mar 1;27(5):1311-1315. doi: 10.1016/j.bmcl.2016.10.009. Epub 2016 Oct 15. Bioorg Med Chem Lett. 2017. PMID: 28169164
Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1).
Kanouni T, Severin C, Cho RW, Yuen NY, Xu J, Shi L, Lai C, Del Rosario JR, Stansfield RK, Lawton LN, Hosfield D, O'Connell S, Kreilein MM, Tavares-Greco P, Nie Z, Kaldor SW, Veal JM, Stafford JA, Chen YK. Kanouni T, et al. J Med Chem. 2020 Dec 10;63(23):14522-14529. doi: 10.1021/acs.jmedchem.0c00978. Epub 2020 Oct 9. J Med Chem. 2020. PMID: 33034194
Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1).
Nie Z, Feher V, Natala S, McBride C, Kiryanov A, Jones B, Lam B, Liu Y, Kaldor S, Stafford J, Hikami K, Uchiyama N, Kawamoto T, Hikichi Y, Matsumoto S, Amano N, Zhang L, Hosfield D, Skene R, Zou H, Cao X, Ichikawa T. Nie Z, et al. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3662-6. doi: 10.1016/j.bmcl.2013.02.083. Epub 2013 Feb 27. Bioorg Med Chem Lett. 2013. PMID: 23664874 Clinical Trial.
36 results