Application of the Bicyclo[1.1.1]pentane Motif as a Nonclassical Phenyl Ring Bioisostere in the Design of a Potent and Orally Active γ-Secretase Inhibitor
Stepan, Antonia F, Subramanyam, Chakrapani, Efremov, Ivan V, Dutra, Jason K, O’Sullivan, Theresa J, DiRico, Kenneth J, McDonald, W. Scott, Won, Annie, Dorff, Peter H, Nolan, Charles E, Becker, Stacey L, Pustilnik, Leslie R, Riddell, David R, Kauffman, Gregory W, Kormos, Bethany L, Zhang, Liming, Lu, Yasong, Capetta, Steven H, Green, Michael E, Karki, Kapil, Sibley, Evelyn, Atchison, Kevin P, Hallgren, Andrew J, Oborski, Christine E, Robshaw, Ashley E, Sneed, Blossom, O’Donnell, Christopher J
Published in Journal of medicinal chemistry (12.04.2012)
Published in Journal of medicinal chemistry (12.04.2012)
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Impact of Apolipoprotein E (ApoE) Polymorphism on Brain ApoE Levels
Riddell, David R, Zhou, Hua, Atchison, Kevin, Warwick, Helen K, Atkinson, Peter J, Jefferson, Julius, Xu, Lin, Aschmies, Suzan, Kirksey, Yolanda, Hu, Yun, Wagner, Erik, Parratt, Adrienne, Xu, Jane, Li, Zhuting, Zaleska, Margaret M, Jacobsen, J. Steve, Pangalos, Menelas N, Reinhart, Peter H
Published in The Journal of neuroscience (05.11.2008)
Published in The Journal of neuroscience (05.11.2008)
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Chemoproteomic profiling reveals that cathepsin D off-target activity drives ocular toxicity of β-secretase inhibitors
Zuhl, Andrea M, Nolan, Charles E, Brodney, Michael A, Niessen, Sherry, Atchison, Kevin, Houle, Christopher, Karanian, David A, Ambroise, Claude, Brulet, Jeffrey W, Beck, Elizabeth M, Doran, Shawn D, O'Neill, Brian T, Am Ende, Christopher W, Chang, Cheng, Geoghegan, Kieran F, West, Graham M, Judkins, Joshua C, Hou, Xinjun, Riddell, David R, Johnson, Douglas S
Published in Nature communications (11.10.2016)
Published in Nature communications (11.10.2016)
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3D Timelapse Analysis of Muscle Satellite Cell Motility
Siegel, Ashley L., Atchison, Kevin, Fisher, Kevin E., Davis, George E., Cornelison, D.D.W.
Published in Stem cells (Dayton, Ohio) (01.10.2009)
Published in Stem cells (Dayton, Ohio) (01.10.2009)
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Acute gamma-secretase inhibition improves contextual fear conditioning in the Tg2576 mouse model of Alzheimer's disease
Comery, Thomas A, Martone, Robert L, Aschmies, Suzan, Atchison, Kevin P, Diamantidis, George, Gong, Xiaohai, Zhou, Hua, Kreft, Anthony F, Pangalos, Menelas N, Sonnenberg-Reines, June, Jacobsen, J Steven, Marquis, Karen L
Published in The Journal of neuroscience (28.09.2005)
Published in The Journal of neuroscience (28.09.2005)
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Enhanced clearance of Aβ in brain by sustaining the plasmin proteolysis cascade
Jacobsen, J. Steven, Comery, Thomas A, Martone, Robert L, Elokdah, Hassan, Crandall, David L, Oganesian, Aram, Aschmies, Suzan, Kirksey, Yolanda, Gonzales, Cathleen, Xu, Jane, Zhou, Hua, Atchison, Kevin, Wagner, Erik, Zaleska, Margaret M, Das, Indranil, Arias, Robert L, Bard, Jonathan, Riddell, David, Gardell, Stephen J, Abou-Gharbia, Magid, Robichaud, Albert, Magolda, Ronald, Vlasuk, George P, Bjornsson, Thorir, Reinhart, Peter H, Pangalos, Menelas N
Published in Proceedings of the National Academy of Sciences - PNAS (24.06.2008)
Published in Proceedings of the National Academy of Sciences - PNAS (24.06.2008)
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( S) -N-(5-Chlorothiophene-2-sulfonyl)-β,β-diethylalaninol a Notch-1-sparing γ-secretase inhibitor
Cole, Derek C., Stock, Joseph R., Kreft, Anthony F., Antane, Madelene, Aschmies, Suzan H., Atchison, Kevin P., Casebier, David S., Comery, Thomas A., Diamantidis, George, Ellingboe, John W., Harrison, Boyd L., Hu, Yun, Jin, Mei, Kubrak, Dennis M., Lu, Peimin, Mann, Charles W., Martone, Robert L., Moore, William J., Oganesian, Aram, Riddell, David R., Sonnenberg-Reines, June, Sun, Shaiu-Ching, Wagner, Erik, Wang, Zheng, Woller, Kevin R., Xu, Zheng, Zhou, Hua, Jacobsen, J. Steven
Published in Bioorganic & medicinal chemistry letters (01.02.2009)
Published in Bioorganic & medicinal chemistry letters (01.02.2009)
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Synthesis and structure–activity relationship of a novel series of heterocyclic sulfonamide γ-secretase inhibitors
Pu, Jun, Kreft, Anthony F., Aschmies, Suzan H., Atchison, Kevin P., Berkowitz, Joshua, Caggiano, Thomas J., Chlenov, Micheal, Diamantidis, George, Harrison, Boyd L., Hu, Yun, Huryn, Donna, Steven Jacobsen, J., Jin, Mei, Lipinski, Kerri, Lu, Peimin, Martone, Robert L., Morris, Koi, Sonnenberg-Reines, June, Riddell, Dave R., Sabalski, Joan, Sun, Shaiu-Ching, Wagner, Erik, Wang, Yiqun, Xu, Zheng, Zhou, Hua, Resnick, Lynn
Published in Bioorganic & medicinal chemistry (01.07.2009)
Published in Bioorganic & medicinal chemistry (01.07.2009)
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Tau molecular diversity contributes to clinical heterogeneity in Alzheimer's disease
Dujardin, Simon, Commins, Caitlin, Lathuiliere, Aurelien, Beerepoot, Pieter, Fernandes, Analiese R, Kamath, Tarun V, De Los Santos, Mark B, Klickstein, Naomi, Corjuc, Diana L, Corjuc, Bianca T, Dooley, Patrick M, Viode, Arthur, Oakley, Derek H, Moore, Benjamin D, Mullin, Kristina, Jean-Gilles, Dinorah, Clark, Ryan, Atchison, Kevin, Moore, Renee, Chibnik, Lori B, Tanzi, Rudolph E, Frosch, Matthew P, Serrano-Pozo, Alberto, Elwood, Fiona, Steen, Judith A, Kennedy, Matthew E, Hyman, Bradley T
Published in Nature medicine (01.08.2020)
Published in Nature medicine (01.08.2020)
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P2-337: Characterization of the affinity of GSI-953 for binding to gamma-secretase and comparison to benchmark gamma-secretase inhibitors
Kreft, Anthony F, Abou-Gharbia, Magid A, Aulabaugh, Ann E, Atchison, Kevin P, Diamantidis, George, Harrison, Boyd L, Hirst, Warren D, Huang, Xinyi, Kubrak, Dennis M, Lipinski, Kerri, Magolda, Ronald L, Martone, Robert L, May, Michael K, Mayer, Scott C, Pangalos, Menelas N, Porte, Alex M, Reinhart, Peter H, Resnick, Lynn, Zhou, Hua, Jacobsen, J. Steven
Published in Alzheimer's & dementia (01.07.2008)
Published in Alzheimer's & dementia (01.07.2008)
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In Vitro and In Vivo Activities of Syn2190, a Novel β-Lactamase Inhibitor
NISHIDA, K, KUNUGITA, C, SALAMA, S. M, ATWAL, H, MICETICH, R. G, UJI, T, HIGASHITANI, F, HYODO, A, UNEMI, N, MAITI, S. N, PHILLIPS, O. A, SPEVAK, P, ATCHISON, K. P
Published in Antimicrobial Agents and Chemotherapy (01.08.1999)
Published in Antimicrobial Agents and Chemotherapy (01.08.1999)
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Abstract 1909: Pan-TGF-β inhibition with PD-1 blockade as a combination treatment strategy to augment anti-tumor immune response in hepatocellular carcinoma
Malkova, Natalia, Theilhaber, Joachim, Levit, Mikhail, Tolstykh, Tatiana, Hebert, Andrew, Atchison, Kevin, Maisonet, Adalis, Sinicropi-Yao, Sara Sara, Protopopov, Alexei, Pollard, Jack, Sidhu, Sukhvinder, Lin, Tun Tun, Pao, Lily, Wiederschain, Dmitri, Sharma, Sharad K.
Published in Cancer research (Chicago, Ill.) (01.07.2021)
Published in Cancer research (Chicago, Ill.) (01.07.2021)
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Abstract 4451: Combination of local mRNA immunotherapy with systemic immune checkpoint blockade demonstrates anti-tumor activity across a diverse range of preclinical syngeneic tumor models
Malkova, Natalia V., Tolstykh, Tatiana, Levit, Mikhail, Theilhaber, Joachim, Hebert, Andrew, Atchison, Kevin, Maisonet, Adalis, Hotz, Christian, Sahin, Ugur, Protopopov, Alexei, Pollard, Jack, Sidhu, Sukhvinder, Wiederschain, Dmitri, Wagenaar, Timothy R.
Published in Cancer research (Chicago, Ill.) (15.08.2020)
Published in Cancer research (Chicago, Ill.) (15.08.2020)
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Utilizing Structures of CYP2D6 and BACE1 Complexes To Reduce Risk of Drug–Drug Interactions with a Novel Series of Centrally Efficacious BACE1 Inhibitors
Brodney, Michael A, Beck, Elizabeth M, Butler, Christopher R, Barreiro, Gabriela, Johnson, Eric F, Riddell, David, Parris, Kevin, Nolan, Charles E, Fan, Ying, Atchison, Kevin, Gonzales, Cathleen, Robshaw, Ashley E, Doran, Shawn D, Bundesmann, Mark W, Buzon, Leanne, Dutra, Jason, Henegar, Kevin, LaChapelle, Erik, Hou, Xinjun, Rogers, Bruce N, Pandit, Jayvardhan, Lira, Ricardo, Martinez-Alsina, Luis, Mikochik, Peter, Murray, John C, Ogilvie, Kevin, Price, Loren, Sakya, Subas M, Yu, Aijia, Zhang, Yong, O’Neill, Brian T
Published in Journal of medicinal chemistry (09.04.2015)
Published in Journal of medicinal chemistry (09.04.2015)
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Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality
Butler, Christopher R, Ogilvie, Kevin, Martinez-Alsina, Luis, Barreiro, Gabriela, Beck, Elizabeth M, Nolan, Charles E, Atchison, Kevin, Benvenuti, Eric, Buzon, Leanne, Doran, Shawn, Gonzales, Cathleen, Helal, Christopher J, Hou, Xinjun, Hsu, Mei-Hui, Johnson, Eric F, Lapham, Kimberly, Lanyon, Lorraine, Parris, Kevin, O’Neill, Brian T, Riddell, David, Robshaw, Ashley, Vajdos, Felix, Brodney, Michael A
Published in Journal of medicinal chemistry (12.01.2017)
Published in Journal of medicinal chemistry (12.01.2017)
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Age-dependent disruption in hippocampal theta oscillation in amyloid-β overproducing transgenic mice
Scott, Liam, Feng, Jianlin, Kiss, Tamás, Needle, Elie, Atchison, Kevin, Kawabe, Thomas T, Milici, Anthony J, Hajós-Korcsok, Éva, Riddell, David, Hajós, Mihály
Published in Neurobiology of aging (01.07.2012)
Published in Neurobiology of aging (01.07.2012)
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Metabolism-Directed Design of Oxetane-Containing Arylsulfonamide Derivatives as γ-Secretase Inhibitors
Stepan, Antonia F, Karki, Kapil, McDonald, W. Scott, Dorff, Peter H, Dutra, Jason K, DiRico, Kenneth J, Won, Annie, Subramanyam, Chakrapani, Efremov, Ivan V, O’Donnell, Christopher J, Nolan, Charles E, Becker, Stacey L, Pustilnik, Leslie R, Sneed, Blossom, Sun, Hao, Lu, Yasong, Robshaw, Ashley E, Riddell, David, O'Sullivan, Theresa J, Sibley, Evelyn, Capetta, Steven, Atchison, Kevin, Hallgren, Andrew J, Miller, Emily, Wood, Anthony, Obach, R. Scott
Published in Journal of medicinal chemistry (24.11.2011)
Published in Journal of medicinal chemistry (24.11.2011)
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Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease
Martone, Robert L, Zhou, Hua, Atchison, Kevin, Comery, Thomas, Xu, Jane Z, Huang, Xinyi, Gong, Xioahai, Jin, Mei, Kreft, Anthony, Harrison, Boyd, Mayer, Scott C, Aschmies, Suzan, Gonzales, Cathleen, Zaleska, Margaret M, Riddell, David R, Wagner, Erik, Lu, Peimin, Sun, Shaiu-Ching, Sonnenberg-Reines, June, Oganesian, Aram, Adkins, Karissa, Leach, Michael W, Clarke, David W, Huryn, Donna, Abou-Gharbia, Magid, Magolda, Ronald, Bard, Jonathan, Frick, Glen, Raje, Sangeeta, Forlow, S Bradley, Balliet, Carrie, Burczynski, Michael E, Reinhart, Peter H, Wan, Hong I, Pangalos, Menelas N, Jacobsen, J Steven
Published in The Journal of pharmacology and experimental therapeutics (01.11.2009)
Published in The Journal of pharmacology and experimental therapeutics (01.11.2009)
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Discovery of a Series of Efficient, Centrally Efficacious BACE1 Inhibitors through Structure-Based Drug Design
Butler, Christopher R, Brodney, Michael A, Beck, Elizabeth M, Barreiro, Gabriela, Nolan, Charles E, Pan, Feng, Vajdos, Felix, Parris, Kevin, Varghese, Alison H, Helal, Christopher J, Lira, Ricardo, Doran, Shawn D, Riddell, David R, Buzon, Leanne M, Dutra, Jason K, Martinez-Alsina, Luis A, Ogilvie, Kevin, Murray, John C, Young, Joseph M, Atchison, Kevin, Robshaw, Ashley, Gonzales, Cathleen, Wang, Jinlong, Zhang, Yong, O’Neill, Brian T
Published in Journal of medicinal chemistry (26.03.2015)
Published in Journal of medicinal chemistry (26.03.2015)
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Author Correction: Tau molecular diversity contributes to clinical heterogeneity in Alzheimer's disease
Dujardin, Simon, Commins, Caitlin, Lathuiliere, Aurelien, Beerepoot, Pieter, Fernandes, Analiese R, Kamath, Tarun V, De Los Santos, Mark B, Klickstein, Naomi, Corjuc, Diana L, Corjuc, Bianca T, Dooley, Patrick M, Viode, Arthur, Oakley, Derek H, Moore, Benjamin D, Mullin, Kristina, Jean-Gilles, Dinorah, Clark, Ryan, Atchison, Kevin, Moore, Renee, Chibnik, Lori B, Tanzi, Rudolph E, Frosch, Matthew P, Serrano-Pozo, Alberto, Elwood, Fiona, Steen, Judith A, Kennedy, Matthew E, Hyman, Bradley T
Published in Nature medicine (01.02.2021)
Published in Nature medicine (01.02.2021)
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