From Fragment Screening to In Vivo Efficacy: Optimization of a Series of 2-Aminoquinolines as Potent Inhibitors of Beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1)
Cheng, Yuan, Judd, Ted C, Bartberger, Michael D, Brown, James, Chen, Kui, Fremeau, Robert T, Hickman, Dean, Hitchcock, Stephen A, Jordan, Brad, Li, Vivian, Lopez, Patricia, Louie, Steven W, Luo, Yi, Michelsen, Klaus, Nixey, Thomas, Powers, Timothy S, Rattan, Claire, Sickmier, E. Allen, St. Jean, David J, Wahl, Robert C, Wen, Paul H, Wood, Stephen
Published in Journal of medicinal chemistry (25.08.2011)
Published in Journal of medicinal chemistry (25.08.2011)
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Structure- and Property-Based Design of Aminooxazoline Xanthenes as Selective, Orally Efficacious, and CNS Penetrable BACE Inhibitors for the Treatment of Alzheimer’s Disease
Huang, Hongbing, La, Daniel S, Cheng, Alan C, Whittington, Douglas A, Patel, Vinod F, Chen, Kui, Dineen, Thomas A, Epstein, Oleg, Graceffa, Russell, Hickman, Dean, Kiang, Y.-H, Louie, Steven, Luo, Yi, Wahl, Robert C, Wen, Paul H, Wood, Stephen, Fremeau, Robert T
Published in Journal of medicinal chemistry (08.11.2012)
Published in Journal of medicinal chemistry (08.11.2012)
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The presenilin-1 familial Alzheimer disease mutant P117L impairs neurogenesis in the hippocampus of adult mice
Wen, Paul H., Hof, Patrick R., Chen, Xiaoping, Gluck, Karen, Austin, Gregory, Younkin, Steven G., Younkin, Linda H., DeGasperi, Rita, Gama Sosa, Miguel A., Robakis, Nikolaos K., Haroutunian, Vahram, Elder, Gregory A.
Published in Experimental neurology (01.08.2004)
Published in Experimental neurology (01.08.2004)
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Discovery of AM-6494: A Potent and Orally Efficacious β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2
Pettus, Liping H, Bourbeau, Matthew P, Bradley, Jodi, Bartberger, Michael D, Chen, Kui, Hickman, Dean, Johnson, Michael, Liu, Qingyian, Manning, James R, Nanez, Adrian, Siegmund, Aaron C, Wen, Paul H, Whittington, Douglas A, Allen, Jennifer R, Wood, Stephen
Published in Journal of medicinal chemistry (12.03.2020)
Published in Journal of medicinal chemistry (12.03.2020)
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Overexpression of Wild Type But Not an FAD Mutant Presenilin-1 Promotes Neurogenesis in the Hippocampus of Adult Mice
Wen, Paul H., Shao, Xiang, Shao, Zhiping, Hof, Patrick R., Wisniewski, Thomas, Kelley, Kevin, Friedrich, Victor L., Ho, Lap, Pasinetti, Giulio M., Shioi, Junichi, Robakis, Nikolaos K., Elder, Gregory A.
Published in Neurobiology of disease (01.06.2002)
Published in Neurobiology of disease (01.06.2002)
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A CBP Binding Transcriptional Repressor Produced by the PS1/ϵ-Cleavage of N-Cadherin Is Inhibited by PS1 FAD Mutations
Marambaud, Philippe, Wen, Paul H, Dutt, Anindita, Shioi, Junichi, Takashima, Akihiko, Siman, Robert, Robakis, Nikolaos K
Published in Cell (05.09.2003)
Published in Cell (05.09.2003)
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Selective expression of presenilin 1 in neural progenitor cells rescues the cerebral hemorrhages and cortical lamination defects in presenilin 1-null mutant mice
Wen, Paul H, De Gasperi, Rita, Sosa, Miguel A Gama, Rocher, Anne B, Friedrich, Jr, Victor L, Hof, Patrick R, Elder, Gregory A
Published in Development (Cambridge) (01.09.2005)
Published in Development (Cambridge) (01.09.2005)
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Inhibitors of β‑Site Amyloid Precursor Protein Cleaving Enzyme (BACE1): Identification of (S)‑7-(2-Fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5′H‑spiro[chromeno[2,3‑b]pyridine-5,4′-oxazol]-2′-amine (AMG-8718)
Dineen, Thomas A, Chen, Kui, Cheng, Alan C, Derakhchan, Katayoun, Epstein, Oleg, Esmay, Joel, Hickman, Dean, Kreiman, Chuck E, Marx, Isaac E, Wahl, Robert C, Wen, Paul H, Weiss, Matthew M, Whittington, Douglas A, Wood, Stephen, Fremeau, Robert T, White, Ryan D, Patel, Vinod F
Published in Journal of medicinal chemistry (11.12.2014)
Published in Journal of medicinal chemistry (11.12.2014)
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The development of a structurally distinct series of BACE1 inhibitors via the (Z)-fluoro-olefin amide bioisosteric replacement
Frohn, Michael, Liu, Longbin, Siegmund, Aaron C., Qian, Wenyuan, Amegadzie, Albert, Chen, Ning, Tan, Helming, Hickman, Dean, Wood, Stephen, Wen, Paul H., Bartberger, Michael D., Whittington, Douglas A., Allen, Jennifer R., Bourbeau, Matthew P.
Published in Bioorganic & medicinal chemistry letters (15.07.2020)
Published in Bioorganic & medicinal chemistry letters (15.07.2020)
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Lead Optimization and Modulation of hERG Activity in a Series of Aminooxazoline Xanthene β‑Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors
Epstein, Oleg, Bryan, Marian C, Cheng, Alan C, Derakhchan, Katayoun, Dineen, Thomas A, Hickman, Dean, Hua, Zihao, Human, Jason B, Kreiman, Charles, Marx, Isaac E, Weiss, Matthew M, Wahl, Robert C, Wen, Paul H, Whittington, Douglas A, Wood, Stephen, Zheng, Xiao Mei, Fremeau, Robert T, White, Ryan D, Patel, Vinod F
Published in Journal of medicinal chemistry (11.12.2014)
Published in Journal of medicinal chemistry (11.12.2014)
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Design and Preparation of a Potent Series of Hydroxyethylamine Containing β-Secretase Inhibitors That Demonstrate Robust Reduction of Central β-Amyloid
Weiss, Matthew M, Williamson, Toni, Babu-Khan, Safura, Bartberger, Michael D, Brown, James, Chen, Kui, Cheng, Yuan, Citron, Martin, Croghan, Michael D, Dineen, Thomas A, Esmay, Joel, Graceffa, Russell F, Harried, Scott S, Hickman, Dean, Hitchcock, Stephen A, Horne, Daniel B, Huang, Hongbing, Imbeah-Ampiah, Ronke, Judd, Ted, Kaller, Matthew R, Kreiman, Charles R, La, Daniel S, Li, Vivian, Lopez, Patricia, Louie, Steven, Monenschein, Holger, Nguyen, Thomas T, Pennington, Lewis D, Rattan, Claire, San Miguel, Tisha, Sickmier, E.Allen, Wahl, Robert C, Wen, Paul H, Wood, Stephen, Xue, Qiufen, Yang, Bryant H, Patel, Vinod F, Zhong, Wenge
Published in Journal of medicinal chemistry (08.11.2012)
Published in Journal of medicinal chemistry (08.11.2012)
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Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer’s disease
Chen, Jian Jeffrey, Liu, Qingyian, Yuan, Chester, Gore, Vijay, Lopez, Patricia, Ma, Vu, Amegadzie, Albert, Qian, Wenyuan, Judd, Ted C., Minatti, Ana E., Brown, James, Cheng, Yuan, Xue, May, Zhong, Wenge, Dineen, Thomas A., Epstein, Oleg, Human, Jason, Kreiman, Charles, Marx, Isaac, Weiss, Matthew M., Hitchcock, Stephen A., Powers, Timothy S., Chen, Kui, Wen, Paul H., Whittington, Douglas A., Cheng, Alan C., Bartberger, Michael D., Hickman, Dean, Werner, Jonathan A., Vargas, Hugo M., Everds, Nancy E., Vonderfecht, Steven L., Dunn, Robert T., Wood, Stephen, Fremeau, Robert T., White, Ryan D., Patel, Vinod F.
Published in Bioorganic & medicinal chemistry letters (15.02.2015)
Published in Bioorganic & medicinal chemistry letters (15.02.2015)
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Journal Article
Design and Synthesis of Potent, Orally Efficacious Hydroxyethylamine Derived β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors
Dineen, Thomas A, Weiss, Matthew M, Williamson, Toni, Acton, Paul, Babu-Khan, Safura, Bartberger, Michael D, Brown, James, Chen, Kui, Cheng, Yuan, Citron, Martin, Croghan, Michael D, Dunn, Robert T, Esmay, Joel, Graceffa, Russell F, Harried, Scott S, Hickman, Dean, Hitchcock, Stephen A, Horne, Daniel B, Huang, Hongbing, Imbeah-Ampiah, Ronke, Judd, Ted, Kaller, Matthew R, Kreiman, Charles R, La, Daniel S, Li, Vivian, Lopez, Patricia, Louie, Steven, Monenschein, Holger, Nguyen, Thomas T, Pennington, Lewis D, San Miguel, Tisha, Sickmier, E. Allen, Vargas, Hugo M, Wahl, Robert C, Wen, Paul H, Whittington, Douglas A, Wood, Stephen, Xue, Qiufen, Yang, Bryant H, Patel, Vinod F, Zhong, Wenge
Published in Journal of medicinal chemistry (08.11.2012)
Published in Journal of medicinal chemistry (08.11.2012)
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An Orally Available BACE1 Inhibitor That Affords Robust CNS Aβ Reduction without Cardiovascular Liabilities
Cheng, Yuan, Brown, James, Judd, Ted C, Lopez, Patricia, Qian, Wenyuan, Powers, Timothy S, Chen, Jian Jeffrey, Bartberger, Michael D, Chen, Kui, Dunn, Robert T, Epstein, Oleg, Fremeau, Robert T, Harried, Scott, Hickman, Dean, Hitchcock, Stephen A, Luo, Yi, Minatti, Ana Elena, Patel, Vinod F, Vargas, Hugo M, Wahl, Robert C, Weiss, Matthew M, Wen, Paul H, White, Ryan D, Whittington, Douglas A, Zheng, Xiao Mei, Wood, Stephen
Published in ACS medicinal chemistry letters (12.02.2015)
Published in ACS medicinal chemistry letters (12.02.2015)
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Establishing the relationship between in vitro potency, pharmacokinetic, and pharmacodynamic parameters in a series of orally available, hydroxyethylamine-derived β-secretase inhibitors
Wood, Stephen, Wen, Paul H, Zhang, Jianhua, Zhu, Li, Luo, Yi, Babu-Khan, Safura, Chen, Kui, Pham, Roger, Esmay, Joel, Dineen, Thomas A, Kaller, Matthew R, Weiss, Matthew M, Hitchcock, Stephen A, Citron, Martin, Zhong, Wenge, Hickman, Dean, Williamson, Toni
Published in The Journal of pharmacology and experimental therapeutics (01.11.2012)
Published in The Journal of pharmacology and experimental therapeutics (01.11.2012)
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Discovery of 2-methylpyridine-based biaryl amides as γ-secretase modulators for the treatment of Alzheimer’s disease
Chen, Jian Jeffrey, Qian, Wenyuan, Biswas, Kaustav, Yuan, Chester, Amegadzie, Albert, Liu, Qingyian, Nixey, Thomas, Zhu, Joe, Ncube, Mqhele, Rzasa, Robert M., Chavez, Frank, Chen, Ning, DeMorin, Frenel, Rumfelt, Shannon, Tegley, Christopher M., Allen, Jennifer R., Hitchcock, Stephen, Hungate, Randy, Bartberger, Michael D., Zalameda, Leeanne, Liu, Yichin, McCarter, John D., Zhang, Jianhua, Zhu, Li, Babu-Khan, Safura, Luo, Yi, Bradley, Jodi, Wen, Paul H., Reid, Darren L., Koegler, Frank, Dean, Charles, Hickman, Dean, Correll, Tiffany L., Williamson, Toni, Wood, Stephen
Published in Bioorganic & medicinal chemistry letters (01.12.2013)
Published in Bioorganic & medicinal chemistry letters (01.12.2013)
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Journal Article
A Potent and Orally Efficacious, Hydroxyethylamine-Based Inhibitor of β-Secretase
Kaller, Matthew R, Harried, Scott S, Albrecht, Brian, Amarante, Patricia, Babu-Khan, Safura, Bartberger, Michael D, Brown, James, Brown, Ryan, Chen, Kui, Cheng, Yuan, Citron, Martin, Croghan, Michael D, Graceffa, Russell, Hickman, Dean, Judd, Ted, Kriemen, Chuck, La, Daniel, Li, Vivian, Lopez, Patricia, Luo, Yi, Masse, Craig, Monenschein, Holger, Nguyen, Thomas, Pennington, Lewis D, Miguel, Tisha San, Sickmier, E. Allen, Wahl, Robert C, Weiss, Matthew M, Wen, Paul H, Williamson, Toni, Wood, Stephen, Xue, May, Yang, Bryant, Zhang, Jianhua, Patel, Vinod, Zhong, Wenge, Hitchcock, Stephen
Published in ACS medicinal chemistry letters (08.11.2012)
Published in ACS medicinal chemistry letters (08.11.2012)
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Journal Article
Cortical development in the presenilin‐1 null mutant mouse fails after splitting of the preplate and is not due to a failure of reelin‐dependent signaling
De Gasperi, Rita, Gama Sosa, Miguel A., Wen, Paul H., Li, Jingjun, Perez, Gissel M., Curran, Tom, Elder, Gregory A.
Published in Developmental dynamics (01.09.2008)
Published in Developmental dynamics (01.09.2008)
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Human midsized neurofilament subunit induces motor neuron disease in transgenic mice
Gama Sosa, Miguel A, Friedrich, Victor L, DeGasperi, Rita, Kelley, Kevin, Wen, Paul H, Senturk, Emir, Lazzarini, Robert A, Elder, Gregory A
Published in Experimental neurology (01.11.2003)
Published in Experimental neurology (01.11.2003)
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Journal Article
Neural progenitor cells do not differentiate prematurely in presenilin-1 null mutant mice
Wen, Paul H., De Gasperi, Rita, Gama Sosa, Miguel A., Elder, Gregory A.
Published in Neuroscience letters (23.11.2004)
Published in Neuroscience letters (23.11.2004)
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