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Novel potent azetidine-based compounds irreversibly inhibit Stat3 activation and induce antitumor response against human breast tumor growth in vivo.
Yue P, Zhu Y, Brotherton-Pleiss C, Fu W, Verma N, Chen J, Nakamura K, Chen W, Chen Y, Alonso-Valenteen F, Mikhael S, Medina-Kauwe L, Kershaw KM, Celeridad M, Pan S, Limpert AS, Sheffler DJ, Cosford NDP, Shiao SL, Tius MA, Lopez-Tapia F, Turkson J. Yue P, et al. Among authors: sheffler dj. Cancer Lett. 2022 May 28;534:215613. doi: 10.1016/j.canlet.2022.215613. Epub 2022 Mar 9. Cancer Lett. 2022. PMID: 35276290 Free PMC article.
Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer.
Ren H, Bakas NA, Vamos M, Chaikuad A, Limpert AS, Wimer CD, Brun SN, Lambert LJ, Tautz L, Celeridad M, Sheffler DJ, Knapp S, Shaw RJ, Cosford NDP. Ren H, et al. Among authors: sheffler dj. J Med Chem. 2020 Dec 10;63(23):14609-14625. doi: 10.1021/acs.jmedchem.0c00873. Epub 2020 Nov 17. J Med Chem. 2020. PMID: 33200929 Free PMC article.
Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia.
Bata N, Chaikuad A, Bakas NA, Limpert AS, Lambert LJ, Sheffler DJ, Berger LM, Liu G, Yuan C, Wang L, Peng Y, Dong J, Celeridad M, Layng F, Knapp S, Cosford NDP. Bata N, et al. Among authors: sheffler dj. J Med Chem. 2022 Jan 27;65(2):1352-1369. doi: 10.1021/acs.jmedchem.1c00804. Epub 2021 Nov 22. J Med Chem. 2022. PMID: 34807584 Free PMC article.
A cellular target engagement assay for the characterization of SHP2 (PTPN11) phosphatase inhibitors.
Romero C, Lambert LJ, Sheffler DJ, De Backer LJS, Raveendra-Panickar D, Celeridad M, Grotegut S, Rodiles S, Holleran J, Sergienko E, Pasquale EB, Cosford NDP, Tautz L. Romero C, et al. Among authors: sheffler dj. J Biol Chem. 2020 Feb 28;295(9):2601-2613. doi: 10.1074/jbc.RA119.010838. Epub 2020 Jan 17. J Biol Chem. 2020. PMID: 31953320 Free PMC article.
Benzodiazepinone derivatives protect against endoplasmic reticulum stress-mediated cell death in human neuronal cell lines.
Zou H, Limpert AS, Zou J, Dembo A, Lee PS, Grant D, Ardecky R, Pinkerton AB, Magnuson GK, Goldman ME, Rong J, Teriete P, Sheffler DJ, Reed JC, Cosford ND. Zou H, et al. Among authors: sheffler dj. ACS Chem Neurosci. 2015 Mar 18;6(3):464-75. doi: 10.1021/cn500297v. Epub 2015 Jan 17. ACS Chem Neurosci. 2015. PMID: 25544056 Free PMC article.
Development and use of a high-throughput screen to identify novel modulators of the corticotropin releasing factor binding protein.
Haass-Koffler CL, Francis TC, Gandhi P, Patel R, Naemuddin M, Nielsen CK, Bartlett SE, Bonci A, Vasile S, Hood BL, Suyama E, Hedrick MP, Smith LH, Limpert AS, Roberto M, Cosford NDP, Sheffler DJ. Haass-Koffler CL, et al. Among authors: sheffler dj. SLAS Discov. 2022 Dec;27(8):448-459. doi: 10.1016/j.slasd.2022.09.005. Epub 2022 Oct 7. SLAS Discov. 2022. PMID: 36210051 Free PMC article.
Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence.
Sidique S, Dhanya RP, Sheffler DJ, Nickols HH, Yang L, Dahl R, Mangravita-Novo A, Smith LH, D'Souza MS, Semenova S, Conn PJ, Markou A, Cosford ND. Sidique S, et al. Among authors: sheffler dj. J Med Chem. 2012 Nov 26;55(22):9434-45. doi: 10.1021/jm3005306. Epub 2012 Oct 23. J Med Chem. 2012. PMID: 23009245 Free PMC article.
63 results