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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.
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.
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.
Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependence.
Dhanya RP, Sheffler DJ, Dahl R, Davis M, Lee PS, Yang L, Nickols HH, Cho HP, Smith LH, D'Souza MS, Conn PJ, Der-Avakian A, Markou A, Cosford ND. Dhanya RP, et al. Among authors: sheffler dj. J Med Chem. 2014 May 22;57(10):4154-72. doi: 10.1021/jm5000563. Epub 2014 May 9. J Med Chem. 2014. PMID: 24735492 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.
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 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.
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.
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