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Pyrazole Ureas as Low Dose, CNS Penetrant Glucosylceramide Synthase Inhibitors for the Treatment of Parkinson's Disease.
Roecker AJ, Schirripa KM, Loughran HM, Tong L, Liang T, Fillgrove KL, Kuo Y, Bleasby K, Collier H, Altman MD, Ford MC, Drolet RE, Cosden M, Jinn S, Hatcher NG, Yao L, Kandebo M, Vardigan JD, Flick RB, Liu X, Minnick C, Price LA, Watt ML, Lemaire W, Burlein C, Adam GC, Austin LA, Marcus JN, Smith SM, Fraley ME. Roecker AJ, et al. Among authors: watt ml. ACS Med Chem Lett. 2023 Jan 12;14(2):146-155. doi: 10.1021/acsmedchemlett.2c00441. eCollection 2023 Feb 9. ACS Med Chem Lett. 2023. PMID: 36793422 Free PMC article.
Fluorinated Isoindolinone-Based Glucosylceramide Synthase Inhibitors with Low Human Dose Projections.
Loughran HM, Schirripa KM, Roecker AJ, Breslin MJ, Tong L, Fillgrove KL, Kuo Y, Bleasby K, Collier H, Altman MD, Ford MC, Newman JA, Drolet RE, Cosden M, Jinn S, Flick RB, Liu X, Minnick C, Watt ML, Lemaire W, Burlein C, Adam GC, Austin LA, Marcus JN, Smith SM, Fraley ME. Loughran HM, et al. Among authors: watt ml. ACS Med Chem Lett. 2023 Dec 21;15(1):123-131. doi: 10.1021/acsmedchemlett.3c00436. eCollection 2024 Jan 11. ACS Med Chem Lett. 2023. PMID: 38229758
A novel glucosylceramide synthase inhibitor attenuates alpha synuclein pathology and lysosomal dysfunction in preclinical models of synucleinopathy.
Cosden M, Jinn S, Yao L, Gretzula CA, Kandebo M, Toolan D, Hatcher NG, Ma L, Lemaire W, Adam GC, Burlein C, Minnick C, Flick R, Watt ML, Mulhearn J, Fraley M, Drolet RE, Marcus JN, Smith SM. Cosden M, et al. Among authors: watt ml. Neurobiol Dis. 2021 Nov;159:105507. doi: 10.1016/j.nbd.2021.105507. Epub 2021 Sep 9. Neurobiol Dis. 2021. PMID: 34509608 Free article.
Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M₁ agonists.
Liu B, Croy CH, Hitchcock SA, Allen JR, Rao Z, Evans D, Bures MG, McKinzie DL, Watt ML, Stuart Gregory G, Hansen MM, Hoogestraat PJ, Jamison JA, Okha-Mokube FM, Stratford RE, Turner W, Bymaster F, Felder CC. Liu B, et al. Among authors: watt ml. Bioorg Med Chem Lett. 2015 Oct 1;25(19):4158-63. doi: 10.1016/j.bmcl.2015.08.011. Epub 2015 Aug 8. Bioorg Med Chem Lett. 2015. PMID: 26299349
PGC-1α, a potential therapeutic target for early intervention in Parkinson's disease.
Zheng B, Liao Z, Locascio JJ, Lesniak KA, Roderick SS, Watt ML, Eklund AC, Zhang-James Y, Kim PD, Hauser MA, Grünblatt E, Moran LB, Mandel SA, Riederer P, Miller RM, Federoff HJ, Wüllner U, Papapetropoulos S, Youdim MB, Cantuti-Castelvetri I, Young AB, Vance JM, Davis RL, Hedreen JC, Adler CH, Beach TG, Graeber MB, Middleton FA, Rochet JC, Scherzer CR; Global PD Gene Expression (GPEX) Consortium. Zheng B, et al. Among authors: watt ml. Sci Transl Med. 2010 Oct 6;2(52):52ra73. doi: 10.1126/scitranslmed.3001059. Sci Transl Med. 2010. PMID: 20926834 Free PMC article.