Search Results - "Stamford, Andrew W."

Design and Validation of Bicyclic Iminopyrimidinones As Beta Amyloid Cleaving Enzyme‑1 (BACE1) Inhibitors: Conformational Constraint to Favor a Bioactive Conformation by 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

“…On the basis of our observation that the biaryl substituent of iminopyrimidinone 7 must be in a pseudoaxial conformation to occupy the contiguous S1–S3…”
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Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV‑1 Protease Inhibitors by 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

“…Using the HIV-1 protease binding mode of MK-8718 and PL-100 as inspiration, a novel aspartate binding bicyclic piperazine sulfonamide core was designed and…”
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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 by 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

“…Antagonism of the adenosine A2A receptor offers great promise in the treatment of Parkinson's disease. Employing the known…”
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The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients by Kennedy, Matthew E, Stamford, Andrew W, Chen, Xia, Cox, Kathleen, Cumming, Jared N, Dockendorf, Marissa F, Egan, Michael, Ereshefsky, Larry, Hodgson, Robert A, Hyde, Lynn A, Jhee, Stanford, Kleijn, Huub J, Kuvelkar, Reshma, Li, Wei, Mattson, Britta A, Mei, Hong, Palcza, John, Scott, Jack D, Tanen, Michael, Troyer, Matthew D, Tseng, Jack L, Stone, Julie A, Parker, Eric M, Forman, Mark S

“…β-Amyloid (Aβ) peptides are thought to be critically involved in the etiology of Alzheimer's disease (AD). The aspartyl protease β-site amyloid precursor…”
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Structure–function analysis of the SHOC2–MRAS–PP1C holophosphatase complex by 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.

“…Receptor tyrosine kinase (RTK)–RAS signalling through the downstream mitogen-activated protein kinase (MAPK) cascade regulates cell proliferation and survival…”
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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 by 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

“…Verubecestat 3 (MK-8931), a diaryl amide-substituted 3-imino-1,2,4-thiadiazinane 1,1-dioxide derivative, is a high-affinity β-site amyloid precursor protein…”
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Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells by 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.

“…[Display omitted] Cancer cells reprogram their metabolism to support growth and to mitigate cellular stressors. The serine synthesis pathway has been…”
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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 by 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

“…Leucine-rich repeat kinase 2 (LRRK2) is a large, multidomain protein which contains a kinase domain and GTPase domain among other regions. Individuals…”
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Small-Molecule Inhibition of the Acyl-Lysine Reader ENL as a Strategy against Acute Myeloid Leukemia by Liu, Yiman, Li, Qinglan, Alikarami, Fatemeh, Barrett, Declan R, Mahdavi, Leila, Li, Hangpeng, Tang, Sylvia, Khan, Tanweer A, Michino, Mayako, Hill, Connor, Song, Lele, Yang, Lu, Li, Yuanyuan, Pokharel, Sheela Pangeni, Stamford, Andrew W, Liverton, Nigel, Renzetti, Louis M, Taylor, Simon, Watt, Gillian F, Ladduwahetty, Tammy, Kargman, Stacia, Meinke, Peter T, Foley, Michael A, Shi, Junwei, Li, Haitao, Carroll, Martin, Chen, Chun-Wei, Gardini, Alessandro, Maillard, Ivan, Huggins, David J, Bernt, Kathrin M, Wan, Liling

“…The chromatin reader eleven-nineteen leukemia (ENL) has been identified as a critical dependency in acute myeloid leukemia (AML), but its therapeutic potential…”
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Targeting eIF4A-Dependent Translation of KRAS Signaling Molecules by Singh, Kamini, Lin, Jianan, Lecomte, Nicolas, Mohan, Prathibha, Gokce, Askan, Sanghvi, Viraj R, Jiang, Man, Grbovic-Huezo, Olivera, Burčul, Antonija, Stark, Stefan G, Romesser, Paul B, Chang, Qing, Melchor, Jerry P, Beyer, Rachel K, Duggan, Mark, Fukase, Yoshiyuki, Yang, Guangli, Ouerfelli, Ouathek, Viale, Agnes, de Stanchina, Elisa, Stamford, Andrew W, Meinke, Peter T, Rätsch, Gunnar, Leach, Steven D, Ouyang, Zhengqing, Wendel, Hans-Guido

“…Pancreatic adenocarcinoma (PDAC) epitomizes a deadly cancer driven by abnormal KRAS signaling. Here, we show that the eIF4A RNA helicase is required for…”
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Recruitment of FBXO22 for targeted degradation of NSD2 by 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

“…Targeted protein degradation (TPD) is an emerging therapeutic strategy that would benefit from new chemical entities with which to recruit a wider variety of…”
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Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor by 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.

“…From an initial lead 1, a structure-based design approach led to identification of a novel, high-affinity iminohydantoin BACE1 inhibitor that lowers…”
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A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors by 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

“…Aberrant gene-silencing through dysregulation of polycomb protein activity has emerged as an important oncogenic mechanism in cancer, implicating polycomb…”
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Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable In Vivo Studies: Discovery of TDI-11055 by 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.

“…Eleven-nineteen leukemia (ENL) is an epigenetic reader protein that drives oncogenic transcriptional programs in acute myeloid leukemia (AML). AML is one of…”
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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 by 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

“…We describe successful efforts to optimize the in vivo profile and address off-target liabilities of a series of BACE1 inhibitors represented by 6 that…”
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Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety by 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

“…Herein we describe structure–activity relationship (SAR) and metabolite identification (Met-ID) studies that provided insight into the origin of time-dependent…”
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Preladenant, a selective A2A receptor antagonist, is active in primate models of movement disorders by 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

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Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders by 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

“…Parkinson's Disease (PD) and Extrapyramidal Syndrome (EPS) are movement disorders that result from degeneration of the dopaminergic input to the striatum and…”
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CNS amyloid-β, soluble APP-α and -β kinetics during BACE inhibition by 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

“…BACE, a β-secretase, is an attractive potential disease-modifying therapeutic strategy for Alzheimer's disease (AD) as it results directly in the decrease of…”
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A Novel Method for the Preparation of 4‑Arylimidazolones by DeMong, Duane E, Ng, Irene, Miller, Michael W, Stamford, Andrew W

“…A series of 4-arylimidazolones have been accessed via late-stage, palladium-mediated arylation of acetone- and cyclohexanone-derived 4-chloroimidazolones. The…”
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