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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.
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.
Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates.
Egan DF, Chun MG, Vamos M, Zou H, Rong J, Miller CJ, Lou HJ, Raveendra-Panickar D, Yang CC, Sheffler DJ, Teriete P, Asara JM, Turk BE, Cosford ND, Shaw RJ. Egan DF, et al. Among authors: sheffler dj. Mol Cell. 2015 Jul 16;59(2):285-97. doi: 10.1016/j.molcel.2015.05.031. Epub 2015 Jun 25. Mol Cell. 2015. PMID: 26118643 Free PMC article.
Identification and Development of a New Positron Emission Tomography Ligand 4-(2-Fluoro-4-[11C]methoxyphenyl)-5-((1-methyl-1H-pyrazol-3-yl)methoxy)picolinamide for Imaging Metabotropic Glutamate Receptor Subtype 2 (mGlu2).
Yamasaki T, Zhang X, Kumata K, Zhang Y, Deng X, Fujinaga M, Chen Z, Mori W, Hu K, Wakizaka H, Hatori A, Xie L, Ogawa M, Nengaki N, Van R, Shao Y, Sheffler DJ, Cosford NDP, Liang SH, Zhang MR. Yamasaki T, et al. Among authors: sheffler dj. J Med Chem. 2020 Oct 22;63(20):11469-11483. doi: 10.1021/acs.jmedchem.9b01991. Epub 2020 Sep 22. J Med Chem. 2020. PMID: 32960052 Free PMC article.
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 and synthesis of an orally active metabotropic glutamate receptor subtype-2 (mGluR2) positive allosteric modulator (PAM) that decreases cocaine self-administration in rats.
Dhanya RP, Sidique S, Sheffler DJ, Nickols HH, Herath A, Yang L, Dahl R, Ardecky R, Semenova S, Markou A, Conn PJ, Cosford ND. Dhanya RP, et al. Among authors: sheffler dj. J Med Chem. 2011 Jan 13;54(1):342-53. doi: 10.1021/jm1012165. Epub 2010 Dec 14. J Med Chem. 2011. PMID: 21155570 Free PMC article.
63 results