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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