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Published in Science translational medicine (02.11.2016)
Published in Science translational medicine (02.11.2016)
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Published in Nature communications (21.05.2019)
Published in Nature communications (21.05.2019)
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Kwon, Jason J., Hajian, Behnoush, Bian, Yuemin, Young, Lucy C., Amor, Alvaro J., Fuller, James R., Fraley, Cara V., Sykes, Abbey M., So, Jonathan, Pan, Joshua, Baker, Laura, Lee, Sun Joo, Wheeler, Douglas B., Mayhew, David L., Persky, Nicole S., Yang, Xiaoping, Root, David E., Barsotti, Anthony M., Stamford, Andrew W., Perry, Charles K., Burgin, Alex, McCormick, Frank, Lemke, Christopher T., Hahn, William C., Aguirre, Andrew J.
Published in Nature (London) (08.09.2022)
Published in Nature (London) (08.09.2022)
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Discovery of the 3‑Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)–A β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer’s Disease
Scott, Jack D, Li, Sarah W, Brunskill, Andrew P. J, Chen, Xia, Cox, Kathleen, Cumming, Jared N, Forman, Mark, Gilbert, Eric J, Hodgson, Robert A, Hyde, Lynn A, Jiang, Qin, Iserloh, Ulrich, Kazakevich, Irina, Kuvelkar, Reshma, Mei, Hong, Meredith, John, Misiaszek, Jeffrey, Orth, Peter, Rossiter, Lana M, Slater, Meagan, Stone, Julie, Strickland, Corey O, Voigt, Johannes H, Wang, Ganfeng, Wang, Hongwu, Wu, Yusheng, Greenlee, William J, Parker, Eric M, Kennedy, Matthew E, Stamford, Andrew W
Published in Journal of medicinal chemistry (08.12.2016)
Published in Journal of medicinal chemistry (08.12.2016)
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Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells
Mullarky, Edouard, Xu, Jiayi, Robin, Anita D., Huggins, David J., Jennings, Andy, Noguchi, Naoyoshi, Olland, Andrea, Lakshminarasimhan, Damodharan, Miller, Michael, Tomita, Daisuke, Michino, Mayako, Su, Taojunfeng, Zhang, Guoan, Stamford, Andrew W., Meinke, Peter T., Kargman, Stacia, Cantley, Lewis C.
Published in Bioorganic & medicinal chemistry letters (01.09.2019)
Published in Bioorganic & medicinal chemistry letters (01.09.2019)
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Discovery of a 3‑(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity
Scott, Jack D, DeMong, Duane E, Greshock, Thomas J, Basu, Kallol, Dai, Xing, Harris, Joel, Hruza, Alan, Li, Sarah W, Lin, Sue-Ing, Liu, Hong, Macala, Megan K, Hu, Zhiyong, Mei, Hong, Zhang, Honglu, Walsh, Paul, Poirier, Marc, Shi, Zhi-Cai, Xiao, Li, Agnihotri, Gautam, Baptista, Marco A. S, Columbus, John, Fell, Matthew J, Hyde, Lynn A, Kuvelkar, Reshma, Lin, Yinghui, Mirescu, Christian, Morrow, John A, Yin, Zhizhang, Zhang, Xiaoping, Zhou, Xiaoping, Chang, Ronald K, Embrey, Mark W, Sanders, John M, Tiscia, Heather E, Drolet, Robert E, Kern, Jonathan T, Sur, Sylvie M, Renger, John J, Bilodeau, Mark T, Kennedy, Matthew E, Parker, Eric M, Stamford, Andrew W, Nargund, Ravi, McCauley, John A, Miller, Michael W
Published in Journal of medicinal chemistry (13.04.2017)
Published in Journal of medicinal chemistry (13.04.2017)
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Targeting eIF4A-Dependent Translation of KRAS Signaling Molecules
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Small-Molecule Inhibition of the Acyl-Lysine Reader ENL as a Strategy against Acute Myeloid Leukemia
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Published in Cancer discovery (02.11.2022)
Published in Cancer discovery (02.11.2022)
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Recruitment of FBXO22 for targeted degradation of NSD2
Nie, David Y, Tabor, John R, Li, Jianping, Kutera, Maria, St-Germain, Jonathan, Hanley, Ronan P, Wolf, Esther, Paulakonis, Ethan, Kenney, Tristan M G, Duan, Shili, Shrestha, Suman, Owens, Dominic D G, Maitland, Matthew E R, Pon, Ailing, Szewczyk, Magdalena, Lamberto, Anthony Joseph, Menes, Michael, Li, Fengling, Penn, Linda Z, Barsyte-Lovejoy, Dalia, Brown, Nicholas G, Barsotti, Anthony M, Stamford, Andrew W, Collins, Jon L, Wilson, Derek J, Raught, Brian, Licht, Jonathan D, James, Lindsey I, Arrowsmith, Cheryl H
Published in Nature chemical biology (04.07.2024)
Published in Nature chemical biology (04.07.2024)
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Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor
Cumming, Jared N., Smith, Elizabeth M., Wang, Lingyan, Misiaszek, Jeffrey, Durkin, James, Pan, Jianping, Iserloh, Ulrich, Wu, Yusheng, Zhu, Zhaoning, Strickland, Corey, Voigt, Johannes, Chen, Xia, Kennedy, Matthew E., Kuvelkar, Reshma, Hyde, Lynn A., Cox, Kathleen, Favreau, Leonard, Czarniecki, Michael F., Greenlee, William J., McKittrick, Brian A., Parker, Eric M., Stamford, Andrew W.
Published in Bioorganic & medicinal chemistry letters (01.04.2012)
Published in Bioorganic & medicinal chemistry letters (01.04.2012)
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A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors
Liang, Rui, Tomita, Daisuke, Sasaki, Yusuke, Ginn, John, Michino, Mayako, Huggins, David J, Baxt, Leigh, Kargman, Stacia, Shahid, Maaz, Aso, Kazuyoshi, Duggan, Mark, Stamford, Andrew W, DeStanchina, Elisa, Liverton, Nigel, Meinke, Peter T, Foley, Michael A, Phillips, Richard E
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Published in ACS medicinal chemistry letters (10.03.2022)
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Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable In Vivo Studies: Discovery of TDI-11055
Michino, Mayako, Khan, Tanweer A., Miller, Michael W., Fukase, Yoshiyuki, Vendome, Jeremie, Adura, Carolina, Glickman, J. Fraser, Liu, Yiman, Wan, Liling, Allis, C. David, Stamford, Andrew W., Meinke, Peter T., Renzetti, Louis M., Kargman, Stacia, Liverton, Nigel J., Huggins, David J.
Published in ACS medicinal chemistry letters (11.04.2024)
Published in ACS medicinal chemistry letters (11.04.2024)
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Structure-Based Design of an Iminoheterocyclic β‑Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates
Mandal, Mihirbaran, Wu, Yusheng, Misiaszek, Jeffrey, Li, Guoqing, Buevich, Alexei, Caldwell, John P, Liu, Xiaoxiang, Mazzola, Robert D, Orth, Peter, Strickland, Corey, Voigt, Johannes, Wang, Hongwu, Zhu, Zhaoning, Chen, Xia, Grzelak, Michael, Hyde, Lynn A, Kuvelkar, Reshma, Leach, Prescott T, Terracina, Giuseppe, Zhang, Lili, Zhang, Qi, Michener, Maria S, Smith, Brad, Cox, Kathleen, Grotz, Diane, Favreau, Leonard, Mitra, Kaushik, Kazakevich, Irina, McKittrick, Brian A, Greenlee, William, Kennedy, Matthew E, Parker, Eric M, Cumming, Jared N, Stamford, Andrew W
Published in Journal of medicinal chemistry (14.04.2016)
Published in Journal of medicinal chemistry (14.04.2016)
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Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety
Mandal, Mihirbaran, Mitra, Kaushik, Grotz, Diane, Lin, Xinjie, Palamanda, Jairam, Kumari, Pramila, Buevich, Alexei, Caldwell, John P, Chen, Xia, Cox, Kathleen, Favreau, Leonard, Hyde, Lynn, Kennedy, Matthew E, Kuvelkar, Reshma, Liu, Xiaoxiang, Mazzola, Robert D, Parker, Eric, Rindgen, Diane, Sherer, Edward, Wang, Hongwu, Zhu, Zhaoning, Stamford, Andrew W, Cumming, Jared N
Published in Journal of medicinal chemistry (13.12.2018)
Published in Journal of medicinal chemistry (13.12.2018)
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Design and Validation of Bicyclic Iminopyrimidinones As Beta Amyloid Cleaving Enzyme‑1 (BACE1) Inhibitors: Conformational Constraint to Favor a Bioactive Conformation
Mandal, Mihirbaran, Zhu, Zhaoning, Cumming, Jared N, Liu, Xiaoxiang, Strickland, Corey, Mazzola, Robert D, Caldwell, John P, Leach, Prescott, Grzelak, Michael, Hyde, Lynn, Zhang, Qi, Terracina, Giuseppe, Zhang, Lili, Chen, Xia, Kuvelkar, Reshma, Kennedy, Matthew E, Favreau, Leonard, Cox, Kathleen, Orth, Peter, Buevich, Alexei, Voigt, Johannes, Wang, Hongwu, Kazakevich, Irina, McKittrick, Brian A, Greenlee, William, Parker, Eric M, Stamford, Andrew W
Published in Journal of medicinal chemistry (08.11.2012)
Published in Journal of medicinal chemistry (08.11.2012)
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Preladenant, a selective A2A receptor antagonist, is active in primate models of movement disorders
HODGSON, Robert A, BEDARD, Paul J, DARE, Aurelie, NEUSTADT, Bernard R, STAMFORD, Andrew W, HUNTER, John C, VARTY, Geoffrey B, KAZDOBA, Tatiana M, DI PAOLO, Therese, GRZELAK, Michael E, POND, Annamarie J, HADJTAHAR, Abdallah, BELANGER, Nancy, GREGOIRE, Laurent
Published in Experimental neurology (01.10.2010)
Published in Experimental neurology (01.10.2010)
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Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders
Hodgson, Robert A, Bedard, Paul J, Varty, Geoffrey B, Kazdoba, Tatiana M, Di Paolo, Therese, Grzelak, Michael E, Pond, Annamarie J, Hadjtahar, Abdallah, Belanger, Nancy, Gregoire, Laurent, Dare, Aurelie, Neustadt, Bernard R, Stamford, Andrew W, Hunter, John C
Published in Experimental neurology (01.10.2010)
Published in Experimental neurology (01.10.2010)
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Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV‑1 Protease Inhibitors
Bungard, Christopher J, Williams, Peter D, Schulz, Jurgen, Wiscount, Catherine M, Holloway, M. Katharine, Loughran, H. Marie, Manikowski, Jesse J, Su, Hua-Poo, Bennett, David J, Chang, Lehua, Chu, Xin-Jie, Crespo, Alejandro, Dwyer, Michael P, Keertikar, Kartik, Morriello, Gregori J, Stamford, Andrew W, Waddell, Sherman T, Zhong, Bin, Hu, Bin, Ji, Tao, Diamond, Tracy L, Bahnck-Teets, Carolyn, Carroll, Steven S, Fay, John F, Min, Xu, Morris, William, Ballard, Jeanine E, Miller, Michael D, McCauley, John A
Published in ACS medicinal chemistry letters (14.12.2017)
Published in ACS medicinal chemistry letters (14.12.2017)
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Potent, selective, and orally active adenosine A2A receptor antagonists : Arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1 ,5-c]pyrimidines
NEUSTADT, Bernard R, JINSONG HAO, FOSTER, Carolyn, ARIK, Leyla, LACHOWICZ, Jean, NG, Kwokei, FENG, Kung-I, LINDO, Neil, GREENLEE, William J, STAMFORD, Andrew W, TULSHIAN, Deen, ONGINI, Ennio, HUNTER, John, MONOPOLI, Angela, BERTORELLI, Rosalia
Published in Bioorganic & medicinal chemistry letters (01.03.2007)
Published in Bioorganic & medicinal chemistry letters (01.03.2007)
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CNS amyloid-β, soluble APP-α and -β kinetics during BACE inhibition
Dobrowolska, Justyna A, Michener, Maria S, Wu, Guoxin, Patterson, Bruce W, Chott, Robert, Ovod, Vitaliy, Pyatkivskyy, Yuriy, Wildsmith, Kristin R, Kasten, Tom, Mathers, Parker, Dancho, Mandy, Lennox, Christina, Smith, Brad E, Gilberto, David, McLoughlin, Debra, Holder, Daniel J, Stamford, Andrew W, Yarasheski, Kevin E, Kennedy, Matthew E, Savage, Mary J, Bateman, Randall J
Published in The Journal of neuroscience (11.06.2014)
Published in The Journal of neuroscience (11.06.2014)
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