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Page 1
Tau: From research to clinical development.
Holtzman DM, Carrillo MC, Hendrix JA, Bain LJ, Catafau AM, Gault LM, Goedert M, Mandelkow E, Mandelkow EM, Miller DS, Ostrowitzki S, Polydoro M, Smith S, Wittmann M, Hutton M. Holtzman DM, et al. Among authors: smith s. Alzheimers Dement. 2016 Oct;12(10):1033-1039. doi: 10.1016/j.jalz.2016.03.018. Epub 2016 May 4. Alzheimers Dement. 2016. PMID: 27154059 Review.
MK-8719, a Novel and Selective O-GlcNAcase Inhibitor That Reduces the Formation of Pathological Tau and Ameliorates Neurodegeneration in a Mouse Model of Tauopathy.
Wang X, Li W, Marcus J, Pearson M, Song L, Smith K, Terracina G, Lee J, Hong KK, Lu SX, Hyde L, Chen SC, Kinsley D, Melchor JP, Rubins DJ, Meng X, Hostetler E, Sur C, Zhang L, Schachter JB, Hess JF, Selnick HG, Vocadlo DJ, McEachern EJ, Uslaner JM, Duffy JL, Smith SM. Wang X, et al. J Pharmacol Exp Ther. 2020 Aug;374(2):252-263. doi: 10.1124/jpet.120.266122. Epub 2020 Jun 3. J Pharmacol Exp Ther. 2020. PMID: 32493725
Discovery of [¹¹C]MK-8193 as a PET tracer to measure target engagement of phosphodiesterase 10A (PDE10A) inhibitors.
Cox CD, Hostetler ED, Flores BA, Evelhoch JL, Fan H, Gantert L, Holahan M, Eng W, Joshi A, McGaughey G, Meng X, Purcell M, Raheem IT, Riffel K, Yan Y, Renger JJ, Smith SM, Coleman PJ. Cox CD, et al. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4893-4898. doi: 10.1016/j.bmcl.2015.05.080. Epub 2015 Jun 1. Bioorg Med Chem Lett. 2015. PMID: 26077491
Preclinical Characterization of the Phosphodiesterase 10A PET Tracer [(11)C]MK-8193.
Hostetler ED, Fan H, Joshi AD, Zeng Z, Eng W, Gantert L, Holahan M, Meng X, Miller P, O'Malley S, Purcell M, Riffel K, Salinas C, Williams M, Ma B, Buist N, Smith SM, Coleman PJ, Cox CD, Flores BA, Raheem IT, Cook JJ, Evelhoch JL. Hostetler ED, et al. Among authors: smith sm. Mol Imaging Biol. 2016 Aug;18(4):579-87. doi: 10.1007/s11307-015-0910-0. Mol Imaging Biol. 2016. PMID: 26596571
LRRK2 inhibition prevents endolysosomal deficits seen in human Parkinson's disease.
Rocha EM, De Miranda BR, Castro S, Drolet R, Hatcher NG, Yao L, Smith SM, Keeney MT, Di Maio R, Kofler J, Hastings TG, Greenamyre JT. Rocha EM, et al. Among authors: smith sm. Neurobiol Dis. 2020 Feb;134:104626. doi: 10.1016/j.nbd.2019.104626. Epub 2019 Oct 13. Neurobiol Dis. 2020. PMID: 31618685 Free PMC article.
Discovery and Optimization of a Series of Pyrimidine-Based Phosphodiesterase 10A (PDE10A) Inhibitors through Fragment Screening, Structure-Based Design, and Parallel Synthesis.
Shipe WD, Sharik SS, Barrow JC, McGaughey GB, Theberge CR, Uslaner JM, Yan Y, Renger JJ, Smith SM, Coleman PJ, Cox CD. Shipe WD, et al. Among authors: smith sm. J Med Chem. 2015 Oct 8;58(19):7888-94. doi: 10.1021/acs.jmedchem.5b00983. Epub 2015 Sep 25. J Med Chem. 2015. PMID: 26378882
Structure-Guided Design and Procognitive Assessment of a Potent and Selective Phosphodiesterase 2A Inhibitor.
Stachel SJ, Berger R, Nomland AB, Ginnetti AT, Paone DV, Wang D, Puri V, Lange H, Drott J, Lu J, Marcus J, Dwyer MP, Suon S, Uslaner JM, Smith SM. Stachel SJ, et al. Among authors: smith sm. ACS Med Chem Lett. 2018 Jul 26;9(8):815-820. doi: 10.1021/acsmedchemlett.8b00214. eCollection 2018 Aug 9. ACS Med Chem Lett. 2018. PMID: 30128073 Free PMC article.
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: smith sm. Neurobiol Dis. 2021 Nov;159:105507. doi: 10.1016/j.nbd.2021.105507. Epub 2021 Sep 9. Neurobiol Dis. 2021. PMID: 34509608 Free article.
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