Zobrazeno 1 - 7 of 7 pro vyhledávání: '"Pearl Tanaka"'
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Discovery of (R)-4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): Metabolically Stable γ-Secretase Inhibitors that Selectively Inhibit the Production of Amyloid-β over Notch
Autor: Anna Liao, Gary Probst, Pamela S. Keim, Kang Hu, Roy K. Hom, David A. Quincy, Michael S. Dappen, Grace T. Kwong, Jenifer Smith, Martin L. Neitzel, Ying-zi Xu, Elizabeth F. Brigham, Kevin P. Quinn, Frédérique Bard, Minghua Sun, Jing Wu, John-Michael Sauer, Dora Kholodenko, Hongbin Zhang, William Wallace, Matthew N. Mattson, Patricia Sacayon, Jacek Jagodzinski, Hing L. Sham, Brian T. Peterson, Simeon Bowers, Jennifer Marugg, Guriqbal S. Basi, Lee H. Latimer, Susanna S. Hemphill, Darren B. Dressen, Karina Wong, Kevin Tanaka, Michael P. Bova, Pamela Santiago, Daniel K. Ness, Anh P. Truong, Wes Zmolek, Lany Ruslim, Christopher Willits, Michael K. Lee, Andrei W. Konradi, Xiaocong M. Ye, Lam Nguyen, Chris M. Semko, Ted A. Yednock, Ruth N. Motter, Albert W. Garofalo, Erich Goldbach, Pearl Tanaka, Danielle L. Aubele
Publikováno v: Journal of Medicinal Chemistry. 56:5261-5274
Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c5b61686f688dd0abd9c5edac66d7201
https://doi.org/10.1021/jm301741t
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3
Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors
Autor: Kevin P. Quinn, Marc Adler, Gary Probst, Albert W. Garofalo, Anh P. Truong, Danny Tam, Erich Goldbach, Danielle L. Aubele, Maurizio Franzini, David Chian, Grace Kwong, Xiaocong M. Ye, Zhao Ren, Hing L. Sham, Lany Ruslim, Pearl Tanaka, Elizabeth F. Brigham, Ruth Motter
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:1974-1977
Mutations in leucine-rich repeat kinase 2 (LRRK2) are associated with familial Parkinson’s disease (PD). The kinase activity of this complex protein is increased by pathogenic mutations. Inhibition of LRRK2 kinase activity has therefore emerged as
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb913a2423fe06417cb2ecd3e68cdbb8
https://doi.org/10.1016/j.bmcl.2013.02.041
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4
Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): metabolically stable γ-secretase Inhibitors that selectively inhibit the production of amyloid-β over Notch
Autor: Gary, Probst, Danielle L, Aubele, Simeon, Bowers, Darren, Dressen, Albert W, Garofalo, Roy K, Hom, Andrei W, Konradi, Jennifer L, Marugg, Matthew N, Mattson, Martin L, Neitzel, Chris M, Semko, Hing L, Sham, Jenifer, Smith, Minghua, Sun, Anh P, Truong, Xiaocong M, Ye, Ying-Zi, Xu, Michael S, Dappen, Jacek J, Jagodzinski, Pamela S, Keim, Brian, Peterson, Lee H, Latimer, David, Quincy, Jing, Wu, Erich, Goldbach, Daniel K, Ness, Kevin P, Quinn, John-Michael, Sauer, Karina, Wong, Hongbin, Zhang, Wes, Zmolek, Elizabeth F, Brigham, Dora, Kholodenko, Kang, Hu, Grace T, Kwong, Michael, Lee, Anna, Liao, Ruth N, Motter, Patricia, Sacayon, Pamela, Santiago, Christopher, Willits, Frédérique, Bard, Michael P, Bova, Susanna S, Hemphill, Lam, Nguyen, Lany, Ruslim, Kevin, Tanaka, Pearl, Tanaka, William, Wallace, Ted A, Yednock, Guriqbal S, Basi
Publikováno v: Journal of medicinal chemistry. 56(13)
Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::109e2b6e92821a752624dca210f7b056
https://pubmed.ncbi.nlm.nih.gov/23713656
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6
P1‐029: A comparison of conventional versus push‐pull microdialysis for the detection of amyloid β in the mouse brain
Autor: Thomas I. F. H. Cremers, Robert Brendza, Ruth Motter, Robert Freije, Marieke G. C. van der Hart, Isaac Veinbergs, Lisa Yu, Harm Kooijker, Pearl Tanaka, Gunnar Flik
Publikováno v: Alzheimer's & Dementia. 7
using a sensitive plate based ELISA system (MSD). Results: Unlike gamma secretase inhibitors, which demonstrate a “potency shift" when the concentration of substrate is very high as in systems overexpressing APP (Burton et al 2008), the potency of
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::922872bd8679497c205fa2a6bf5df9a9
https://doi.org/10.1016/j.jalz.2011.05.309
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