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Discovery of indole-derived pyridopyrazine-1,6-dione γ-secretase modulators that target presenilin.
Pettersson M, Johnson DS, Humphrey JM, Am Ende CW, Evrard E, Efremov I, Kauffman GW, Stepan AF, Stiff CM, Xie L, Bales KR, Hajos-Korcsok E, Murrey HE, Pustilnik LR, Steyn SJ, Wood KM, Verhoest PR. Pettersson M, et al. Among authors: humphrey jm. Bioorg Med Chem Lett. 2015 Feb 15;25(4):908-13. doi: 10.1016/j.bmcl.2014.12.059. Epub 2014 Dec 25. Bioorg Med Chem Lett. 2015. PMID: 25582600
Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability.
Pettersson M, Johnson DS, Humphrey JM, Butler TW, Am Ende CW, Fish BA, Green ME, Kauffman GW, Mullins PB, O'Donnell CJ, Stepan AF, Stiff CM, Subramanyam C, Tran TP, Vetelino BC, Yang E, Xie L, Bales KR, Pustilnik LR, Steyn SJ, Wood KM, Verhoest PR. Pettersson M, et al. Among authors: humphrey jm. ACS Med Chem Lett. 2015 Apr 3;6(5):596-601. doi: 10.1021/acsmedchemlett.5b00070. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005540 Free PMC article.
Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy.
Pettersson M, Johnson DS, Rankic DA, Kauffman GW, Am Ende CW, Butler TW, Boscoe B, Evrard E, Helal CJ, Humphrey JM, Stepan AF, Stiff CM, Yang E, Xie L, Bales KR, Hajos-Korcsok E, Jenkinson S, Pettersen B, Pustilnik LR, Ramirez DS, Steyn SJ, Wood KM, Verhoest PR. Pettersson M, et al. Among authors: humphrey jm. Medchemcomm. 2016 Nov 2;8(4):730-743. doi: 10.1039/c6md00406g. eCollection 2017 Apr 1. Medchemcomm. 2016. PMID: 30108792 Free PMC article.
Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE.
Seneviratne U, Huang Z, Am Ende CW, Butler TW, Cleary L, Dresselhaus E, Evrard E, Fisher EL, Green ME, Helal CJ, Humphrey JM, Lanyon LF, Marconi M, Mukherjee P, Sciabola S, Steppan CM, Sylvain EK, Tuttle JB, Verhoest PR, Wager TT, Xie L, Ramaswamy G, Johnson DS, Pettersson M. Seneviratne U, et al. Among authors: humphrey jm. Cell Chem Biol. 2021 Feb 18;28(2):148-157.e7. doi: 10.1016/j.chembiol.2020.09.002. Epub 2020 Sep 29. Cell Chem Biol. 2021. PMID: 32997975 Free article.
Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.
Helal CJ, Arnold E, Boyden T, Chang C, Chappie TA, Fisher E, Hajos M, Harms JF, Hoffman WE, Humphrey JM, Pandit J, Kang Z, Kleiman RJ, Kormos BL, Lee CW, Lu J, Maklad N, McDowell L, McGinnis D, O'Connor RE, O'Donnell CJ, Ogden A, Piotrowski M, Schmidt CJ, Seymour PA, Ueno H, Vansell N, Verhoest PR, Yang EX. Helal CJ, et al. Among authors: humphrey jm. J Med Chem. 2018 Feb 8;61(3):1001-1018. doi: 10.1021/acs.jmedchem.7b01466. Epub 2018 Jan 16. J Med Chem. 2018. PMID: 29293004
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
Helal CJ, Arnold EP, Boyden TL, Chang C, Chappie TA, Fennell KF, Forman MD, Hajos M, Harms JF, Hoffman WE, Humphrey JM, Kang Z, Kleiman RJ, Kormos BL, Lee CW, Lu J, Maklad N, McDowell L, Mente S, O'Connor RE, Pandit J, Piotrowski M, Schmidt AW, Schmidt CJ, Ueno H, Verhoest PR, Yang EX. Helal CJ, et al. Among authors: humphrey jm. J Med Chem. 2017 Jul 13;60(13):5673-5698. doi: 10.1021/acs.jmedchem.7b00397. Epub 2017 Jun 16. J Med Chem. 2017. PMID: 28574706
55 results