Preparation and biological evaluation of conformationally constrained BACE1 inhibitors
Winneroski, Leonard L., Schiffler, Matthew A., Erickson, Jon A., May, Patrick C., Monk, Scott A., Timm, David E., Audia, James E., Beck, James P., Boggs, Leonard N., Borders, Anthony R., Boyer, Robert D., Brier, Richard A., Hudziak, Kevin J., Klimkowski, Valentine J., Garcia Losada, Pablo, Mathes, Brian M., Stout, Stephanie L., Watson, Brian M., Mergott, Dustin J.
Published in Bioorganic & medicinal chemistry (01.07.2015)
Published in Bioorganic & medicinal chemistry (01.07.2015)
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Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor
May, Patrick C, Dean, Robert A, Lowe, Stephen L, Martenyi, Ferenc, Sheehan, Scott M, Boggs, Leonard N, Monk, Scott A, Mathes, Brian M, Mergott, Dustin J, Watson, Brian M, Stout, Stephanie L, Timm, David E, Smith Labell, Elizabeth, Gonzales, Celedon R, Nakano, Masako, Jhee, Stanford S, Yen, Mark, Ereshefsky, Larry, Lindstrom, Terry D, Calligaro, David O, Cocke, Patrick J, Greg Hall, D, Friedrich, Stuart, Citron, Martin, Audia, James E
Published in The Journal of neuroscience (16.11.2011)
Published in The Journal of neuroscience (16.11.2011)
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The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans
May, Patrick C, Willis, Brian A, Lowe, Stephen L, Dean, Robert A, Monk, Scott A, Cocke, Patrick J, Audia, James E, Boggs, Leonard N, Borders, Anthony R, Brier, Richard A, Calligaro, David O, Day, Theresa A, Ereshefsky, Larry, Erickson, Jon A, Gevorkyan, Hykop, Gonzales, Celedon R, James, Douglas E, Jhee, Stanford S, Komjathy, Steven F, Li, Linglin, Lindstrom, Terry D, Mathes, Brian M, Martényi, Ferenc, Sheehan, Scott M, Stout, Stephanie L, Timm, David E, Vaught, Grant M, Watson, Brian M, Winneroski, Leonard L, Yang, Zhixiang, Mergott, Dustin J
Published in The Journal of neuroscience (21.01.2015)
Published in The Journal of neuroscience (21.01.2015)
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Assessment of Transporter Polymorphisms as a Factor in a BCRP Drug Interaction Study With Lanabecestat
Willis, Brian A, Andersen, Scott W, Ayan-Oshodi, Mosun, James, Douglas E, Liffick, Emily, Hillgren, Kathleen, Guo, Yingying, Monk, Scott A
Published in Journal of clinical pharmacology (01.01.2020)
Published in Journal of clinical pharmacology (01.01.2020)
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Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor
McKinzie, David L, Winneroski, Leonard L, Green, Steven J, Hembre, Erik J, Erickson, Jon A, Willis, Brian A, Monk, Scott A, Aluise, Christopher D, Baker, Thomas K, Lopez, Jose E, Hendle, Jörg, Beck, James P, Brier, Richard A, Boggs, Leonard N, Borders, Anthony R, Cocke, Patrick J, Garcia-Losada, Pablo, Lowe, Stephen L, Mathes, Brian M, May, Patrick C, Porter, Warren J, Stout, Stephanie L, Timm, David E, Watson, Brian M, Yang, Zhixiang, Mergott, Dustin J
Published in Journal of medicinal chemistry (24.06.2021)
Published in Journal of medicinal chemistry (24.06.2021)
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Clinically Negligible Pharmacokinetic and Pharmacodynamic Interactions Between Lanabecestat and Dabigatran Etexilate, a Prototypical P-gp Substrate
Monk, Scott A, Kugler, Alan R, Andersen, Scott W, Ayan-Oshodi, Mosun A, James, Douglas E, Mullen, Jamie, Zimmer, Jennifer A, Willis, Brian A
Published in Journal of clinical pharmacology (01.05.2020)
Published in Journal of clinical pharmacology (01.05.2020)
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Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints
Winneroski, Leonard L., Erickson, Jon A., Green, Steven J., Lopez, Jose E., Stout, Stephanie L., Porter, Warren J., Timm, David E., Audia, James E., Barberis, Mario, Beck, James P., Boggs, Leonard N., Borders, Anthony R., Boyer, Robert D., Brier, Richard A., Hembre, Erik J., Hendle, Jörg, Garcia-Losada, Pablo, Minguez, Jose Miguel, Mathes, Brian M., May, Patrick C., Monk, Scott A., Rankovic, Zoran, Shi, Yuan, Watson, Brian M., Yang, Zhixiang, Mergott, Dustin J.
Published in Bioorganic & medicinal chemistry (01.01.2020)
Published in Bioorganic & medicinal chemistry (01.01.2020)
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Clinical Bioavailability of the Novel BACE1 Inhibitor Lanabecestat (AZD3293): Assessment of Tablet Formulations Versus an Oral Solution and the Impact of Gastric pH on Pharmacokinetics
Ye, Naidong, Monk, Scott A., Daga, Pankaj, Bender, David M., Rosen, Laura B., Mullen, Jamie, Minkwitz, Margaret C., Kugler, Alan R.
Published in Clinical pharmacology in drug development (01.03.2018)
Published in Clinical pharmacology in drug development (01.03.2018)
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Robust Pharmacodynamic Effect of LY3202626, a Central Nervous System Penetrant, Low Dose BACE1 Inhibitor, in Humans and Nonclinical Species
Willis, Brian A., Lowe, Stephen L., Monk, Scott A., Cocke, Patrick J., Aluise, Christopher D., Boggs, Leonard N., Borders, Anthony R., Brier, Richard A., Dean, Robert A., Green, Steven J., James, Douglas E., Jhee, Stanford S., Lin, Qun, Lo, Albert C., May, Patrick C., Watson, Brian M., Winneroski, Leonard L., Yang, Zhixiang, Zimmer, Jennifer A., McKinzie, David L., Mergott, Dustin J.
Published in JAD reports (01.01.2022)
Published in JAD reports (01.01.2022)
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A CORRELATIONAL ANALYSIS OF EXPOSURE AND PHARMACODYNAMIC EFFECTS OF THE BACE1 INHIBITOR LY3202626 IN PDAPP MICE FOLLOWING ACUTE ORAL DOSING
Boggs, Leonard N, May, Patrick C, Yang, Zhixiang, Brier, Richard A, Monk, Scott A, Borders, Anthony R, Winneroski, Leonard L, Green, Steven J, Mergott, Dustin J, McKinzie, David L
Published in Alzheimer's & dementia (01.07.2016)
Published in Alzheimer's & dementia (01.07.2016)
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NONCLINICAL PHARMACOLOGICAL CHARACTERIZATION OF THE BACE1 INHIBITOR LY3202626
McKinzie, David L, May, Patrick C, Boggs, Leonard N, Yang, Zhixiang, Brier, Richard A, Monk, Scott A, Willis, Brian A, Borders, Anthony R, Winneroski, Leonard L, Green, Steven J, Mergott, Dustin J
Published in Alzheimer's & dementia (01.07.2016)
Published in Alzheimer's & dementia (01.07.2016)
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COMBINATION THERAPY WITH A PLAQUE-SPECIFIC ABETA ANTIBODY AND A BACE INHIBITOR RESULTS IN DRAMATIC PLAQUE REDUCTION IN A DOSE-DEPENDENT MANNER IN AGED PDAPP TRANSGENIC MICE
Hole, Justin T, Racke, Margaret M, Tzaferis, John A, Liu, Feng, Oluoch, Herold, Ahmed, Zeshan, Fisher, Alice, Anderson, Wesley, Iversent, Philip, Gonzales, Celedon, Yang, Zhixiang, Boggs, Leonard N, Monk, Scott A, Mergott, Dustin J, Yang, Ying YT, Lu, Jirong, Irizarry, Michael C, Sims, John R, May, Patrick C, Hutton, Michael, Nordstedt, Christer, DeMattos, Ronald B
Published in Alzheimer's & dementia (01.07.2016)
Published in Alzheimer's & dementia (01.07.2016)
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A COMPARISON OF IN VIVO POTENCY IN TWO BACE INHIBITORS AS DETERMINED IN HUMANS AND DOGS
Willis, Brian A, May, Patrick C, Monk, Scott A, Lowe, Stephen L, Friedrich, Stuart, Mergott, Dustin J, Boggs, Leonard, Gevorkyan, Hakop, Jhee, Stan, Dean, Robert A, Nakano, Masako, Gonzales, Celedon R
Published in Alzheimer's & dementia (01.07.2014)
Published in Alzheimer's & dementia (01.07.2014)
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Investigation of dose-responses and longitudinal effects of combination therapy with a plaque-specific amyloid beta antibody and bace inhibitor in aged transgenic mice
DeMattos, Ronald B, Racke, Margaret M, Hole, Justin T, Tzaferis, John A, Liu, Feng, Ahmed, Zeshan, Fisher, Alice, Day, Theresa A, Anderson, Wesley, Iversent, Philip, Gonzales, Celedon, Yang, Zhixiang, Boggs, Leonard, Monk, Scott A, Mergott, Dustin J, Yang, Ying Y.T, Lu, Jirong, Irizarry, Michael C, Sims, John R, May, Patrick C, Hutton, Michael L, Nordstedt, Christer
Published in Alzheimer's & dementia (01.07.2015)
Published in Alzheimer's & dementia (01.07.2015)
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Central and Peripheral Pharmacokinetic and Pharmacodynamic Effects of the β-site APP Cleavage Enzyme (BACE1) Inhibitor LY2811376 In Humans
Martenyi, Ferenc, Lowe, Stephen, Dean, Robert A, Monk, Scott A, Gonzales, Celedon R, Friedrich, Stuart, May, Patrick C, Audia, James E, Citron, Martin, LaBell, Elizabeth S, Moran, Samira, Yen, Mark, Jhee, Stanford, Kam, Jeanelle, Ereshefsky, Larry
Published in Alzheimer's & dementia (01.07.2010)
Published in Alzheimer's & dementia (01.07.2010)
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Reversible stepwise negative regulation of CYP1A1 in cultured rat epidermal cells
Monk, Scott A, Denison, Michael S, Rice, Robert H
Published in Archives of biochemistry and biophysics (15.11.2003)
Published in Archives of biochemistry and biophysics (15.11.2003)
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A single ascending dose study in healthy volunteers to assess the safety and PK of LY3372689, an inhibitor of O‐GlcNAcase (OGA) enzyme: Human/Human trials: Anti‐tau
Kielbasa, William, Phipps, Krista M, Tseng, James, Natanegara, Fanni, Cheng, Eden, Monk, Scott A., Bundgaard, Christoffer, Kevin, Donnelly B., Nuthall, Hugh Norman, McDonald, Nicholas, Lindsay‐Scott, Peter, Dreyfus, Nicolas, Hawk, Mai Khanh, Warner, Susan, Biglan, Kevin, Gilmore, Julie A., Zhang, Xiaoyu, Mergott, Dustin J., Lowe, Stephen L.
Published in Alzheimer's & dementia (01.12.2020)
Published in Alzheimer's & dementia (01.12.2020)
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Journal Article
A single ascending dose study in healthy volunteers to assess the safety and PK of LY3372689, an inhibitor of O‐GlcNAcase (OGA) enzyme
Kielbasa, William, Phipps, Krista M, Tseng, James, Natanegara, Fanni, Cheng, Eden, Monk, Scott A., Bundgaard, Christoffer, Kevin, Donnelly B., Nuthall, Hugh Norman, McDonald, Nicholas, Lindsay‐Scott, Peter, Dreyfus, Nicolas, Hawk, Mai Khanh, Warner, Susan, Biglan, Kevin, Gilmore, Julie A., Zhang, Xiaoyu, Mergott, Dustin J., Lowe, Stephen L.
Published in Alzheimer's & dementia (01.12.2020)
Published in Alzheimer's & dementia (01.12.2020)
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P1‐039: LANABECESTAT DOES NOT AFFECT PHARMACOKINETICS OF THE BCRP SUBSTRATE ROSUVASTATIN
Monk, Scott A., Andersen, Scott W., Ayan-Oshodi, Mosun, Guo, Yingying, Hillgren, Kathleen M., James, Douglas E., Liffick, Emily, Willis, Brian A.
Published in Alzheimer's & dementia (01.07.2018)
Published in Alzheimer's & dementia (01.07.2018)
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