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The AKT modulator A-443654 reduces α-synuclein expression and normalizes ER stress and autophagy.
Gandelman M, Dansithong W, Kales SC, Paul S, Maag G, Aoyama E, Zakharov A, Rai G, Dexheimer T, Whitehill BM, Sun H, Jadhav A, Simeonov A, Henderson MJ, Huynh DP, Pulst SM, Scoles DR. Gandelman M, et al. Among authors: henderson mj. J Biol Chem. 2021 Oct;297(4):101191. doi: 10.1016/j.jbc.2021.101191. Epub 2021 Sep 11. J Biol Chem. 2021. PMID: 34520759 Free PMC article.
Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds.
Horton JR, Liu X, Gale M, Wu L, Shanks JR, Zhang X, Webber PJ, Bell JSK, Kales SC, Mott BT, Rai G, Jansen DJ, Henderson MJ, Urban DJ, Hall MD, Simeonov A, Maloney DJ, Johns MA, Fu H, Jadhav A, Vertino PM, Yan Q, Cheng X. Horton JR, et al. Among authors: henderson mj. Cell Chem Biol. 2016 Jul 21;23(7):769-781. doi: 10.1016/j.chembiol.2016.06.006. Epub 2016 Jul 14. Cell Chem Biol. 2016. PMID: 27427228 Free PMC article.
Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays.
Urban DJ, Martinez NJ, Davis MI, Brimacombe KR, Cheff DM, Lee TD, Henderson MJ, Titus SA, Pragani R, Rohde JM, Liu L, Fang Y, Karavadhi S, Shah P, Lee OW, Wang A, McIver A, Zheng H, Wang X, Xu X, Jadhav A, Simeonov A, Shen M, Boxer MB, Hall MD. Urban DJ, et al. Among authors: henderson mj. Sci Rep. 2017 Oct 6;7(1):12758. doi: 10.1038/s41598-017-12630-x. Sci Rep. 2017. PMID: 28986582 Free PMC article.
Connecting Neuronal Cell Protective Pathways and Drug Combinations in a Huntington's Disease Model through the Application of Quantitative Systems Pharmacology.
Pei F, Li H, Henderson MJ, Titus SA, Jadhav A, Simeonov A, Cobanoglu MC, Mousavi SH, Shun T, McDermott L, Iyer P, Fioravanti M, Carlisle D, Friedlander RM, Bahar I, Taylor DL, Lezon TR, Stern AM, Schurdak ME. Pei F, et al. Among authors: henderson mj. Sci Rep. 2017 Dec 19;7(1):17803. doi: 10.1038/s41598-017-17378-y. Sci Rep. 2017. PMID: 29259176 Free PMC article.
Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A.
Horton JR, Liu X, Wu L, Zhang K, Shanks J, Zhang X, Rai G, Mott BT, Jansen DJ, Kales SC, Henderson MJ, Pohida K, Fang Y, Hu X, Jadhav A, Maloney DJ, Hall MD, Simeonov A, Fu H, Vertino PM, Yan Q, Cheng X. Horton JR, et al. Among authors: henderson mj. J Med Chem. 2018 Apr 12;61(7):3193-3208. doi: 10.1021/acs.jmedchem.8b00261. Epub 2018 Mar 23. J Med Chem. 2018. PMID: 29537847 Free PMC article.
High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2.
Coussens NP, Kales SC, Henderson MJ, Lee OW, Horiuchi KY, Wang Y, Chen Q, Kuznetsova E, Wu J, Chakka S, Cheff DM, Cheng KC, Shinn P, Brimacombe KR, Shen M, Simeonov A, Lal-Nag M, Ma H, Jadhav A, Hall MD. Coussens NP, et al. Among authors: henderson mj. J Biol Chem. 2018 Aug 31;293(35):13750-13765. doi: 10.1074/jbc.RA118.004274. Epub 2018 Jun 26. J Biol Chem. 2018. PMID: 29945974 Free PMC article.
KDM5 histone demethylases repress immune response via suppression of STING.
Wu L, Cao J, Cai WL, Lang SM, Horton JR, Jansen DJ, Liu ZZ, Chen JF, Zhang M, Mott BT, Pohida K, Rai G, Kales SC, Henderson MJ, Hu X, Jadhav A, Maloney DJ, Simeonov A, Zhu S, Iwasaki A, Hall MD, Cheng X, Shadel GS, Yan Q. Wu L, et al. Among authors: henderson mj. PLoS Biol. 2018 Aug 6;16(8):e2006134. doi: 10.1371/journal.pbio.2006134. eCollection 2018 Aug. PLoS Biol. 2018. PMID: 30080846 Free PMC article.
Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A.
Horton JR, Woodcock CB, Chen Q, Liu X, Zhang X, Shanks J, Rai G, Mott BT, Jansen DJ, Kales SC, Henderson MJ, Cyr M, Pohida K, Hu X, Shah P, Xu X, Jadhav A, Maloney DJ, Hall MD, Simeonov A, Fu H, Vertino PM, Cheng X. Horton JR, et al. Among authors: henderson mj. J Med Chem. 2018 Dec 13;61(23):10588-10601. doi: 10.1021/acs.jmedchem.8b01219. Epub 2018 Nov 15. J Med Chem. 2018. PMID: 30392349 Free PMC article.
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
Clausse V, Tao D, Debnath S, Fang Y, Tagad HD, Wang Y, Sun H, LeClair CA, Mazur SJ, Lane K, Shi ZD, Vasalatiy O, Eells R, Baker LK, Henderson MJ, Webb MR, Shen M, Hall MD, Appella E, Appella DH, Coussens NP. Clausse V, et al. Among authors: henderson mj. J Biol Chem. 2019 Nov 15;294(46):17654-17668. doi: 10.1074/jbc.RA119.010201. Epub 2019 Sep 3. J Biol Chem. 2019. PMID: 31481464 Free PMC article.
243 results