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Page 1
Discovery of Phospholipase D Inhibitors with Improved Drug-like Properties and Central Nervous System Penetrance.
May-Dracka TL, Gao F, Hopkins BT, Hronowski X, Chen T, Chodaparambil JV, Metrick CM, Cullivan M, Enyedy I, Kaliszczak M, Kankel MW, Marx I, Michell-Robinson MA, Murugan P, Kumar PR, Rooney M, Schuman E, Sen A, Wang T, Ye T, Peterson EA. May-Dracka TL, et al. Among authors: enyedy i. ACS Med Chem Lett. 2022 Mar 3;13(4):665-673. doi: 10.1021/acsmedchemlett.1c00682. eCollection 2022 Apr 14. ACS Med Chem Lett. 2022. PMID: 35450377 Free PMC article.
Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity.
May-Dracka TL, Arduini R, Bertolotti-Ciarlet A, Bhisetti G, Brickelmaier M, Cahir-McFarland E, Enyedy I, Fontenot JD, Hesson T, Little K, Lyssikatos J, Marcotte D, McKee T, Murugan P, Patterson T, Peng H, Rushe M, Silvian L, Spilker K, Wu P, Xin Z, Burkly LC. May-Dracka TL, et al. Among authors: enyedy i. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1964-1971. doi: 10.1016/j.bmcl.2018.03.032. Epub 2018 Mar 26. Bioorg Med Chem Lett. 2018. PMID: 29636220
Human PLD structures enable drug design and characterization of isoenzyme selectivity.
Metrick CM, Peterson EA, Santoro JC, Enyedy IJ, Murugan P, Chen T, Michelsen K, Cullivan M, Spilker KA, Kumar PR, May-Dracka TL, Chodaparambil JV. Metrick CM, et al. Among authors: enyedy ij. Nat Chem Biol. 2020 Apr;16(4):391-399. doi: 10.1038/s41589-019-0458-4. Epub 2020 Feb 10. Nat Chem Biol. 2020. PMID: 32042197
Discovery of CNS-Penetrant Apoptosis Signal-Regulating Kinase 1 (ASK1) Inhibitors.
Xin Z, Himmelbauer MK, Jones JH, Enyedy I, Gilfillan R, Hesson T, King K, Marcotte DJ, Murugan P, Santoro JC, Gonzalez-Lopez de Turiso F. Xin Z, et al. Among authors: enyedy i. ACS Med Chem Lett. 2020 Feb 12;11(4):485-490. doi: 10.1021/acsmedchemlett.9b00611. eCollection 2020 Apr 9. ACS Med Chem Lett. 2020. PMID: 32292554 Free PMC article.
Discovery of Potent, Selective, and Brain-Penetrant Apoptosis Signal-Regulating Kinase 1 (ASK1) Inhibitors that Modulate Brain Inflammation In Vivo.
Jones JH, Xin Z, Himmelbauer M, Dechantsreiter M, Enyedy I, Hedde J, Fang T, Coomaraswamy J, King KW, Murugan P, Santoro JC, Hesson T, Walther DM, Wei R, Zheng F, Marcotte DJ, Spilker K, Kumar PR, Liu Y, Gilfillan R, Gonzalez-Lopez de Turiso F. Jones JH, et al. Among authors: enyedy i. J Med Chem. 2021 Oct 28;64(20):15402-15419. doi: 10.1021/acs.jmedchem.1c01458. Epub 2021 Oct 15. J Med Chem. 2021. PMID: 34653340
Elucidation of the GSK3α Structure Informs the Design of Novel, Paralog-Selective Inhibitors.
Amaral B, Capacci A, Anderson T, Tezer C, Bajrami B, Lulla M, Lucas B, Chodaparambil JV, Marcotte D, Kumar PR, Murugan P, Spilker K, Cullivan M, Wang T, Peterson AC, Enyedy I, Ma B, Chen T, Yousaf Z, Calhoun M, Golonzhka O, Dillon GM, Koirala S. Amaral B, et al. Among authors: enyedy i. ACS Chem Neurosci. 2023 Mar 15;14(6):1080-1094. doi: 10.1021/acschemneuro.2c00476. Epub 2023 Feb 22. ACS Chem Neurosci. 2023. PMID: 36812145 Free PMC article.
Identification of orally available naphthyridine protein kinase D inhibitors.
Meredith EL, Ardayfio O, Beattie K, Dobler MR, Enyedy I, Gaul C, Hosagrahara V, Jewell C, Koch K, Lee W, Lehmann H, McKinsey TA, Miranda K, Pagratis N, Pancost M, Patnaik A, Phan D, Plato C, Qian M, Rajaraman V, Rao C, Rozhitskaya O, Ruppen T, Shi J, Siska SJ, Springer C, van Eis M, Vega RB, von Matt A, Yang L, Yoon T, Zhang JH, Zhu N, Monovich LG. Meredith EL, et al. Among authors: enyedy i. J Med Chem. 2010 Aug 12;53(15):5400-21. doi: 10.1021/jm100075z. J Med Chem. 2010. PMID: 20684591
Structure-based design of low-nanomolar PIM kinase inhibitors.
Ishchenko A, Zhang L, Le Brazidec JY, Fan J, Chong JH, Hingway A, Raditsis A, Singh L, Elenbaas B, Hong VS, Marcotte D, Silvian L, Enyedy I, Chao J. Ishchenko A, et al. Among authors: enyedy i. Bioorg Med Chem Lett. 2015 Feb 1;25(3):474-80. doi: 10.1016/j.bmcl.2014.12.041. Epub 2014 Dec 19. Bioorg Med Chem Lett. 2015. PMID: 25575657
Discovery of biaryl carboxylamides as potent RORγ inverse agonists.
Chao J, Enyedy I, Van Vloten K, Marcotte D, Guertin K, Hutchings R, Powell N, Jones H, Bohnert T, Peng CC, Silvian L, Hong VS, Little K, Banerjee D, Peng L, Taveras A, Viney JL, Fontenot J. Chao J, et al. Among authors: enyedy i. Bioorg Med Chem Lett. 2015 Aug 1;25(15):2991-7. doi: 10.1016/j.bmcl.2015.05.026. Epub 2015 May 23. Bioorg Med Chem Lett. 2015. PMID: 26048806
52 results