Zobrazeno 1 - 10 of 31 pro vyhledávání: '"Pamela S. Keim"'
1
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 (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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4
Discovery of sulfonamide-pyrazole gamma-secretase inhibitors
Autor: Guriqbal S. Basi, Hongbin Zhang, Pamela S. Keim, Michael A. Pleiss, Martin L. Neitzel, Erich Goldbach, Semko Christopher M, David A. Quincy, Albert W. Garofalo, Andrei W. Konradi, John-Michael Sauer, Matthew N. Mattson, Hing L. Sham, Elizabeth F. Brigham
Publikováno v: Bioorganicmedicinal chemistry letters. 20(7)
Utilizing a pharmacophore hypothesis, previously described gamma-secretase inhibiting HTS hits were evolved into novel tricyclic sulfonamide-pyrazoles, with high in vitro potency, good brain penetration, low metabolic stability, and high clearance.
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c0bbae13a02ac5307da21f3ab0837c81
https://pubmed.ncbi.nlm.nih.gov/20206516
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6
Exact cleavage site of Alzheimer amyloid precursor in neuronal PC-12 cells
Autor: Frederick Esch, Nikolaos K. Robakis, Kumar Sambamurti, Pamela S. Keim, John P. Anderson, Ivan Lieberburg
Publikováno v: Neuroscience Letters. 128:126-128
We have identified the secretory cleavage site in the Alzheimer amyloid precursor (APP) in a non-transfected neuronal cell line, using cyanogen bromide digests of APP purified from medium conditioned by PC-12 cells which were differentiated to a neur
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4696f12e642b072b81445be79c19fc8a
https://doi.org/10.1016/0304-3940(91)90775-o
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9
Cleavage of amyloid beta peptide during constitutive processing of its precursor
Autor: Russell W. Blacher, Donald McClure, Eric C. Beattie, Tilman Oltersdorf, Frederick Esch, Pamela S. Keim, Alan R. Culwell, Pamela J. Ward
Publikováno v: Science (New York, N.Y.). 248(4959)
The amyloid beta peptide (A beta P) is a small fragment of the much larger, broadly distributed amyloid precursor protein (APP). Abundant A beta P deposition in the brains of patients with Alzheimer's disease suggests that altered APP processing may
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::61d919fa82f1eaa7e414e53db86a5011
https://pubmed.ncbi.nlm.nih.gov/2111583
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