Restricted Location of PSEN2/γ-Secretase Determines Substrate Specificity and Generates an Intracellular Aβ Pool
Sannerud, Ragna, Esselens, Cary, Ejsmont, Paulina, Mattera, Rafael, Rochin, Leila, Tharkeshwar, Arun Kumar, De Baets, Greet, De Wever, Veerle, Habets, Roger, Baert, Veerle, Vermeire, Wendy, Michiels, Christine, Groot, Arjan J., Wouters, Rosanne, Dillen, Katleen, Vints, Katlijn, Baatsen, Pieter, Munck, Sebastian, Derua, Rita, Waelkens, Etienne, Basi, Guriqbal S., Mercken, Mark, Vooijs, Marc, Bollen, Mathieu, Schymkowitz, Joost, Rousseau, Frederic, Bonifacino, Juan S., Van Niel, Guillaume, De Strooper, Bart, Annaert, Wim
Published in Cell (30.06.2016)
Published in Cell (30.06.2016)
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Evidence that enzyme processivity mediates differential Aβ production by PS1 and PS2
Pintchovski, Sean A, Schenk, Dale B, Basi, Guriqbal S
Published in Current Alzheimer research (01.01.2013)
Published in Current Alzheimer research (01.01.2013)
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Treatment strategies targeting amyloid β-protein
Schenk, Dale, Basi, Guriqbal S, Pangalos, Menelas N
Published in Cold Spring Harbor perspectives in medicine (01.09.2012)
Published in Cold Spring Harbor perspectives in medicine (01.09.2012)
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Polo-like Kinase 2 (PLK2) Phosphorylates α-Synuclein at Serine 129 in Central Nervous System
Inglis, Kelly J., Chereau, David, Brigham, Elizabeth F., Chiou, San-San, Schöbel, Susanne, Frigon, Normand L., Yu, Mei, Caccavello, Russell J., Nelson, Seth, Motter, Ruth, Wright, Sarah, Chian, David, Santiago, Pamela, Soriano, Ferdie, Ramos, Carla, Powell, Kyle, Goldstein, Jason M., Babcock, Michael, Yednock, Ted, Bard, Frederique, Basi, Guriqbal S., Sham, Hing, Chilcote, Tamie J., McConlogue, Lisa, Griswold-Prenner, Irene, Anderson, John P.
Published in The Journal of biological chemistry (30.01.2009)
Published in The Journal of biological chemistry (30.01.2009)
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Lysine 624 of the amyloid precursor protein (APP) is a critical determinant of amyloid β peptide length: support for a sequential model of γ-secretase intramembrane proteolysis and regulation by the amyloid β precursor protein (APP) juxtamembrane region
Kukar, Thomas L, Ladd, Thomas B, Robertson, Paul, Pintchovski, Sean A, Moore, Brenda, Bann, Maralyssa A, Ren, Zhao, Jansen-West, Karen, Malphrus, Kim, Eggert, Simone, Maruyama, Hiroko, Cottrell, Barbara A, Das, Pritam, Basi, Guriqbal S, Koo, Edward H, Golde, Todd E
Published in The Journal of biological chemistry (18.11.2011)
Published in The Journal of biological chemistry (18.11.2011)
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Crystal structure reveals conservation of amyloid-β conformation recognized by 3D6 following humanization to bapineuzumab
Feinberg, Hadar, Saldanha, José W, Diep, Linnea, Goel, Amita, Widom, Angela, Veldman, Geertruida M, Weis, William I, Schenk, Dale, Basi, Guriqbal S
Published in Alzheimer's research & therapy (02.06.2014)
Published in Alzheimer's research & therapy (02.06.2014)
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Accelerating drug discovery for Alzheimer's disease: best practices for preclinical animal studies
Shineman, Diana W, Basi, Guriqbal S, Bizon, Jennifer L, Colton, Carol A, Greenberg, Barry D, Hollister, Beth A, Lincecum, John, Leblanc, Gabrielle G, Lee, Linda Bobbi H, Luo, Feng, Morgan, Dave, Morse, Iva, Refolo, Lorenzo M, Riddell, David R, Scearce-Levie, Kimberly, Sweeney, Patrick, Yrjänheikki, Juha, Fillit, Howard M
Published in Alzheimer's research & therapy (28.09.2011)
Published in Alzheimer's research & therapy (28.09.2011)
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Purification and cloning of amyloid precursor protein β-secretase from human brain
Sinha, Sukanto, Anderson, John P, Barbour, Robin, Basi, Guriqbal S, Caccavello, Russell, Davis, David, Doan, Minhtam, Dovey, Harry F, Frigon, Normand, Hong, Jin, Jacobson-Croak, Kirsten, Jewett, Nancy, Keim, Pamela, Knops, Jeroen, Lieberburg, Ivan, Power, Michael, Tan, Hua, Tatsuno, Gwen, Tung, Jay, Schenk, Dale, Seubert, Peter, Suomensaari, Susanna M, Wang, Shuwen, Walker, Donald, Zhao, Jun, McConlogue, Lisa, John, Varghese
Published in Nature (London) (02.12.1999)
Published in Nature (London) (02.12.1999)
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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
Probst, Gary, Aubele, Danielle L, Bowers, Simeon, Dressen, Darren, Garofalo, Albert W, Hom, Roy K, Konradi, Andrei W, Marugg, Jennifer L, Mattson, Matthew N, Neitzel, Martin L, Semko, Chris M, Sham, Hing L, Smith, Jenifer, Sun, Minghua, Truong, Anh P, Ye, Xiaocong M, Xu, Ying-zi, Dappen, Michael S, Jagodzinski, Jacek J, Keim, Pamela S, Peterson, Brian, Latimer, Lee H, Quincy, David, Wu, Jing, Goldbach, Erich, Ness, Daniel K, Quinn, Kevin P, Sauer, John-Michael, Wong, Karina, Zhang, Hongbin, Zmolek, Wes, Brigham, Elizabeth F, Kholodenko, Dora, Hu, Kang, Kwong, Grace T, Lee, Michael, Liao, Anna, Motter, Ruth N, Sacayon, Patricia, Santiago, Pamela, Willits, Christopher, Bard, Frédérique, Bova, Michael P, Hemphill, Susanna S, Nguyen, Lam, Ruslim, Lany, Tanaka, Kevin, Tanaka, Pearl, Wallace, William, Yednock, Ted A, Basi, Guriqbal S
Published in Journal of medicinal chemistry (11.07.2013)
Published in Journal of medicinal chemistry (11.07.2013)
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Structural Correlates of Antibodies Associated with Acute Reversal of Amyloid β-related Behavioral Deficits in a Mouse Model of Alzheimer Disease
Basi, Guriqbal S., Feinberg, Hadar, Oshidari, Farshid, Anderson, John, Barbour, Robin, Baker, Jeanne, Comery, Thomas A., Diep, Linnea, Gill, Davinder, Johnson-Wood, Kelly, Goel, Amita, Grantcharova, Katerina, Lee, Mike, Li, Jingzhi, Partridge, Anthony, Griswold-Prenner, Irene, Piot, Nicolas, Walker, Don, Widom, Angela, Pangalos, Menelas N., Seubert, Peter, Jacobsen, J. Steven, Schenk, Dale, Weis, William I.
Published in The Journal of biological chemistry (29.01.2010)
Published in The Journal of biological chemistry (29.01.2010)
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Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors
Ye, Xiaocong M., Konradi, Andrei W., Sun, Minghua, Yuan, Shendong, Aubele, Danielle L., Dappen, Michael, Dressen, Darren, Garofalo, Albert W., Jagodzinski, Jacek J., Latimer, Lee, Probst, Gary D., Sham, Hing L., Wone, David, Xu, Ying-zi, Ness, Daniel, Brigham, Elizabeth, Kwong, Grace T., Willtis, Chris, Tonn, George, Goldbach, Erich, Quinn, Kevin P., Zhang, Hongbin H., Sauer, John-Michael, Bova, Michael, Basi, Guriqbal S.
Published in Bioorganic & medicinal chemistry letters (15.02.2013)
Published in Bioorganic & medicinal chemistry letters (15.02.2013)
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Discovery of sulfonamide–pyrazole γ-secretase inhibitors
Mattson, Matthew N., Neitzel, Martin L., Quincy, David A., Semko, Christopher M., Garofalo, Albert W., Keim, Pamela S., Konradi, Andrei W., Pleiss, Michael A., Sham, Hing L., Brigham, Elizabeth F., Goldbach, Erich G., Zhang, Hongbin, Sauer, John-Michael, Basi, Guriqbal S.
Published in Bioorganic & medicinal chemistry letters (01.04.2010)
Published in Bioorganic & medicinal chemistry letters (01.04.2010)
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Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and Efficacious γ-Secretase Inhibitors
Ye, Xiaocong M., Konradi, Andrei W., Smith, Jenifer, Xu, Ying-Zi, Dressen, Darren, Garofalo, Albert W., Marugg, Jennifer, Sham, Hing L., Truong, Anh P., Jagodzinski, Jacek, Pleiss, Michael, Zhang, Hongbin, Goldbach, Erich, Sauer, John-Michael, Brigham, Elizabeth, Bova, Michael, Basi, Guriqbal S.
Published in Bioorganic & medicinal chemistry letters (01.04.2010)
Published in Bioorganic & medicinal chemistry letters (01.04.2010)
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Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious γ-secretase inhibitors (Part II)
Ye, Xiaocong M., Konradi, Andrei W., Smith, Jenifer, Aubele, Danielle L., Garofalo, Albert W., Marugg, Jennifer, Neitzel, Marty L., Semko, Chris M., Sham, Hing L., Sun, Minghua, Truong, Anh P., Wu, Jing, Zhang, Hongbin, Goldbach, Erich, Sauer, John-Michael, Brigham, Elizabeth F., Bova, Michael, Basi, Guriqbal S.
Published in Bioorganic & medicinal chemistry letters (15.06.2010)
Published in Bioorganic & medicinal chemistry letters (15.06.2010)
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N-Bridged bicyclic sulfonamides as inhibitors of γ-secretase
Bowers, Simeon, Probst, Gary D., Truong, Anh P., Hom, Roy K., Konradi, Andrei W., Sham, Hing L., Garofalo, Albert W., Wong, Karina, Goldbach, Erich, Quinn, Kevin P., Sauer, John-Michael, Wallace, William, Nguyen, Lan, Hemphill, Susanna S., Bova, Michael P., Basi, Guriqbal S.
Published in Bioorganic & medicinal chemistry letters (15.12.2009)
Published in Bioorganic & medicinal chemistry letters (15.12.2009)
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Caspase-mediated Cleavage of DNA Topoisomerase I at Unconventional Sites during Apoptosis
Samejima, K, Svingen, P A, Basi, G S, Kottke, T, Mesner, Jr, P W, Stewart, L, Durrieu, F, Poirier, G G, Alnemri, E S, Champoux, J J, Kaufmann, S H, Earnshaw, W C
Published in The Journal of biological chemistry (12.02.1999)
Published in The Journal of biological chemistry (12.02.1999)
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Pharmacokinetic and pharmacodynamic analysis of a novel gamma secretase inhibitor in a non-transgenic A-beta mouse efficacy model
Quinn, Kevin P, Kuwabara-Wagg, Jonathan, Brigham, Elizabeth, Cabrera, Cristian, Goldbach, Erich, Dreyer, Mark, Hu, Kang, Lee, Mike, Green, Michelle, Ness, Daniel, Santiago, Pamela, Samant, Bhushan, Soriano, Ferdie, Webb, Steve, Basi, Guriqbal S, Sauer, John-Michael
Published in Alzheimer's & dementia (01.07.2009)
Published in Alzheimer's & dementia (01.07.2009)
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Pharmacokinetic and pharmacodynamic analysis of a novel gamma secretase inhibitor in a nontransgenic A-beta mouse efficacy model
Quinn, Kevin P, Kuwabara-Wagg, Jonathan, Brigham, Elizabeth, Cabrera, Cristian, Goldbach, Erich, Dreyer, Mark, Hu, Kang, Lee, Mike, Green, Michelle, Ness, Daniel, Santiago, Pamela, Samant, Bhushan, Soriano, Ferdie, Webb, Steve, Basi, Guriqbal S, Sauer, John-Michael
Published in Alzheimer's & dementia (01.07.2009)
Published in Alzheimer's & dementia (01.07.2009)
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Journal Article
Discovery of ( R )-4-Cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1 H -pyrazolo[4,3- c ]quinoline (ELND006) and ( R )-4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2 H -pyrazolo[4,3- c ]quinoline (ELND007): Metabolically Stable γ-Secretase Inhibitors that Selectively Inhibit the Production of Amyloid-β over Notch
Probst, Gary, Aubele, Danielle L., Bowers, Simeon, Dressen, Darren, Garofalo, Albert W., Hom, Roy K., Konradi, Andrei W., Marugg, Jennifer L., Mattson, Matthew N., Neitzel, Martin L., Semko, Chris M., Sham, Hing L., Smith, Jenifer, Sun, Minghua, Truong, Anh P., Ye, Xiaocong M., Xu, Ying-zi, Dappen, Michael S., Jagodzinski, Jacek J., Keim, Pamela S., Peterson, Brian, Latimer, Lee H., Quincy, David, Wu, Jing, Goldbach, Erich, Ness, Daniel K., Quinn, Kevin P., Sauer, John-Michael, Wong, Karina, Zhang, Hongbin, Zmolek, Wes, Brigham, Elizabeth F., Kholodenko, Dora, Hu, Kang, Kwong, Grace T., Lee, Michael, Liao, Anna, Motter, Ruth N., Sacayon, Patricia, Santiago, Pamela, Willits, Christopher, Bard, Frédérique, Bova, Michael P., Hemphill, Susanna S., Nguyen, Lam, Ruslim, Lany, Tanaka, Kevin, Tanaka, Pearl, Wallace, William, Yednock, Ted A., Basi, Guriqbal S.
Published in Journal of medicinal chemistry (11.07.2013)
Published in Journal of medicinal chemistry (11.07.2013)
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