Michael Siu, Ph.D. - Publications

Affiliations: 
2002 Harvard University, Cambridge, MA, United States 
Area:
synthesis of natural products

20 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2020 Xu J, Carrera DE, Beaudry D, Siu M, Huestis MP, Liu W, Angelaud R, Gosselin F. Fit-for-purpose synthesis of dual leucine zipper kinase (DLK) inhibitor GNE-834 Tetrahedron Letters. 152430. DOI: 10.1016/J.Tetlet.2020.152430  0.393
2018 Siu M, Sengupta Ghosh A, Lewcock JW. Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration. Journal of Medicinal Chemistry. PMID 29863360 DOI: 10.1021/Acs.Jmedchem.8B00370  0.366
2017 Patel S, Meilandt WJ, Erickson RI, Chen J, Deshmukh G, Estrada AA, Fuji RN, Gibbons P, Gustafson A, Harris SF, Imperio J, Liu W, Liu X, Liu Y, Lyssikatos JP, ... ... Siu M, et al. Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease. Journal of Medicinal Chemistry. PMID 28929759 DOI: 10.1021/Acs.Jmedchem.7B00843  0.405
2017 Le Pichon CE, Meilandt WJ, Dominguez S, Solanoy H, Lin H, Ngu H, Gogineni A, Sengupta Ghosh A, Jiang Z, Lee SH, Maloney J, Gandham VD, Pozniak CD, Wang B, Lee S, ... Siu M, et al. Loss of dual leucine zipper kinase signaling is protective in animal models of neurodegenerative disease. Science Translational Medicine. 9. PMID 28814543 DOI: 10.1126/Scitranslmed.Aag0394  0.328
2017 Larhammar M, Huntwork-Rodriguez S, Jiang Z, Solanoy H, Sengupta Ghosh A, Wang B, Kaminker JS, Huang K, Eastham-Anderson J, Siu M, Modrusan Z, Farley MM, Tessier-Lavigne M, Lewcock JW, Watkins TA. Dual leucine zipper kinase-dependent PERK activation contributes to neuronal degeneration following insult. Elife. 6. PMID 28440222 DOI: 10.7554/Elife.20725  0.302
2017 Takahashi RH, Halladay JS, Siu M, Chen Y, Hop CE, Khojasteh SC, Ma S. Novel Mechanism of Decyanation of GDC-0425 by Cytochrome P450. Drug Metabolism and Disposition: the Biological Fate of Chemicals. PMID 28188299 DOI: 10.1124/Dmd.116.074336  0.313
2015 Patel S, Harris SF, Gibbons P, Deshmukh G, Gustafson A, Kellar T, Lin H, Liu X, Liu Y, Liu Y, Ma C, Scearce-Levie K, Ghosh AS, Shin YG, Solanoy H, ... ... Siu M, et al. Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12). Journal of Medicinal Chemistry. PMID 26431428 DOI: 10.1021/Acs.Jmedchem.5B01072  0.389
2015 Patel S, Cohen F, Dean BJ, De La Torre K, Deshmukh G, Estrada AA, Ghosh AS, Gibbons P, Gustafson A, Huestis MP, Le Pichon CE, Lin H, Liu W, Liu X, Liu Y, ... ... Siu M, et al. Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models. Journal of Medicinal Chemistry. 58: 401-18. PMID 25341110 DOI: 10.1021/Jm5013984  0.391
2014 Thomas AA, Hunt KW, Newhouse B, Watts RJ, Liu X, Vigers G, Smith D, Rhodes SP, Brown KD, Otten JN, Burkard M, Cox AA, Geck Do MK, Dutcher D, Rana S, ... ... Siu M, et al. 8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors. Journal of Medicinal Chemistry. 57: 10112-29. PMID 25411915 DOI: 10.1021/Jm5015132  0.341
2014 Volgraf M, Chan L, Huestis MP, Purkey HE, Burkard M, Geck Do M, Harris J, Hunt KW, Liu X, Lyssikatos JP, Rana S, Thomas AA, Vigers GP, Siu M. Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors. Bioorganic & Medicinal Chemistry Letters. 24: 2477-80. PMID 24780121 DOI: 10.1016/J.Bmcl.2014.04.012  0.351
2014 Takahashi R, Ma S, Deese A, Yue Q, Kim-Kang H, Yi Y, Siu M, Hunt KW, Kallan NC, Hop CE, Liu X, Khojasteh SC. Elucidating the mechanism of cytochrome P450-mediated pyrimidine ring conversion to pyrazole metabolites with the BACE1 inhibitor GNE-892 in rats. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 42: 890-8. PMID 24595682 DOI: 10.1124/Dmd.114.057141  0.346
2014 Thomas AA, Hunt KW, Volgraf M, Watts RJ, Liu X, Vigers G, Smith D, Sammond D, Tang TP, Rhodes SP, Metcalf AT, Brown KD, Otten JN, Burkard M, Cox AA, ... ... Siu M, et al. Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system. Journal of Medicinal Chemistry. 57: 878-902. PMID 24397738 DOI: 10.1021/Jm401635N  0.355
2013 Siu M, Pastor R, Liu W, Barrett K, Berry M, Blair WS, Chang C, Chen JZ, Eigenbrot C, Ghilardi N, Gibbons P, He H, Hurley CA, Kenny JR, Cyrus Khojasteh S, et al. 2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors. Bioorganic & Medicinal Chemistry Letters. 23: 5014-21. PMID 23870430 DOI: 10.1016/J.Bmcl.2013.06.008  0.335
2013 Hunt KW, Cook AW, Watts RJ, Clark CT, Vigers G, Smith D, Metcalf AT, Gunawardana IW, Burkard M, Cox AA, Geck Do MK, Dutcher D, Thomas AA, Rana S, Kallan NC, ... ... Siu M, et al. Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species. Journal of Medicinal Chemistry. 56: 3379-403. PMID 23537249 DOI: 10.1021/Jm4002154  0.324
2013 Huestis MP, Liu W, Volgraf M, Purkey HE, Yu C, Wang W, Smith D, Vigers G, Dutcher D, Hunt KW, Siu M. Diethylaminosulfur trifluoride-mediated intramolecular cyclization of 2-hydroxycycloalkylureas to fused bicyclic aminooxazoline compounds and evaluation of their biochemical activity against β-secretase-1 (BACE-1) Tetrahedron Letters. 54: 5802-5807. DOI: 10.2210/Pdb4L7G/Pdb  0.302
2013 Olivero AG, Heffron TP, Baumgardner M, Belvin M, Ross LB, Blaquiere N, Bradley E, Castanedo G, Derynck M, Do S, Dotson J, Dudley D, Edgar K, Folkes A, Francis R, ... ... Siu M, et al. Abstract DDT02-01: Discovery of GDC-0032: A beta-sparing PI3K inhibitor active against PIK3CA mutant tumors. Cancer Research. 73. DOI: 10.1158/1538-7445.Am2013-Ddt02-01  0.391
2012 Hanan EJ, van Abbema A, Barrett K, Blair WS, Blaney J, Chang C, Eigenbrot C, Flynn S, Gibbons P, Hurley CA, Kenny JR, Kulagowski J, Lee L, Magnuson SR, Morris C, ... ... Siu M, et al. Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors. Journal of Medicinal Chemistry. 55: 10090-107. PMID 23061660 DOI: 10.1021/Jm3012239  0.377
2011 Staben ST, Siu M, Goldsmith R, Olivero AG, Do S, Burdick DJ, Heffron TP, Dotson J, Sutherlin DP, Zhu BY, Tsui V, Le H, Lee L, Lesnick J, Lewis C, et al. Structure-based design of thienobenzoxepin inhibitors of PI3-kinase. Bioorganic & Medicinal Chemistry Letters. 21: 4054-8. PMID 21636270 DOI: 10.1016/J.Bmcl.2011.04.124  0.349
2002 Myers AG, Siu M, Ren F. Enantioselective synthesis of (-)-terpestacin and (-)-fusaproliferin: clarification of optical rotational measurements and absolute configurational assignments establishes a homochiral structural series. Journal of the American Chemical Society. 124: 4230-2. PMID 11960450 DOI: 10.1021/Ja020072L  0.521
2002 Myers AG, Siu M. Lewis acid mediated control of allylic epoxide opening in carbocyclization and halide addition pathways Tetrahedron. 58: 6397-6404. DOI: 10.1016/S0040-4020(02)00653-1  0.478
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