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221 results

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Page 1
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: murugan p. 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: murugan p. 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: murugan p. 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 and Brain-Penetrant Tau Tubulin Kinase 1 (TTBK1) Inhibitors that Lower Tau Phosphorylation In Vivo.
Halkina T, Henderson JL, Lin EY, Himmelbauer MK, Jones JH, Nevalainen M, Feng J, King K, Rooney M, Johnson JL, Marcotte DJ, Chodaparambil JV, Kumar PR, Patterson TA, Murugan P, Schuman E, Wong L, Hesson T, Lamore S, Bao C, Calhoun M, Certo H, Amaral B, Dillon GM, Gilfillan R, de Turiso FG. Halkina T, et al. Among authors: murugan p. J Med Chem. 2021 May 13;64(9):6358-6380. doi: 10.1021/acs.jmedchem.1c00382. Epub 2021 May 4. J Med Chem. 2021. PMID: 33944571
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: murugan p. 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
Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.
Hopkins BT, Bame E, Bajrami B, Black C, Bohnert T, Boiselle C, Burdette D, Burns JC, Delva L, Donaldson D, Grater R, Gu C, Hoemberger M, Johnson J, Kapadnis S, King K, Lulla M, Ma B, Marx I, Magee T, Meissner R, Metrick CM, Mingueneau M, Murugan P, Otipoby KL, Polack E, Poreci U, Prince R, Roach AM, Rowbottom C, Santoro JC, Schroeder P, Tang H, Tien E, Zhang F, Lyssikatos J. Hopkins BT, et al. Among authors: murugan p. J Med Chem. 2022 Jan 27;65(2):1206-1224. doi: 10.1021/acs.jmedchem.1c00926. Epub 2021 Nov 4. J Med Chem. 2022. PMID: 34734694
Corrigendum to "Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors" [Bioorg. Med. Chem. Lett. 60 (2022) 128549].
Ma B, Metrick CM, Gu C, Hoemberger M, Bajrami B, Bame E, Huang J, Mingueneau M, Murugan P, Nevalainen M, Santoro JC, Tang H, Wang T, Hopkins BT. Ma B, et al. Among authors: murugan p. Bioorg Med Chem Lett. 2022 Sep 15;72:128856. doi: 10.1016/j.bmcl.2022.128856. Epub 2022 Jun 18. Bioorg Med Chem Lett. 2022. PMID: 35728998 No abstract available.
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: murugan p. 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.
221 results