Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints

Authors: 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.

Source: In Bioorganic & Medicinal Chemistry 1 January 2020 28(1)

Preparation and biological evaluation of conformationally constrained BACE1 inhibitors

Authors: 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.

Source: In Bioorganic & Medicinal Chemistry 1 July 2015 23(13):3260-3268

Robust Pharmacodynamic Effect of LY3202626, a Central Nervous System Penetrant, Low Dose BACE1 Inhibitor, in Humans and Nonclinical Species

Authors: 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.

Source: Journal of Alzheimer's Disease Reports; October 2022, Vol. 6 Issue: 1 p1-15, 15p

A CORRELATIONAL ANALYSIS OF EXPOSURE AND PHARMACODYNAMIC EFFECTS OF THE BACE1 INHIBITOR LY3202626 IN PDAPP MICE FOLLOWING ACUTE ORAL DOSING

Authors: 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.

Source: Alzheimer's & dementia. 15(7):P831-P831

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100093004276.0x000001&indx=1&recIds=ETOCvdc_100093004276.0x000001

NONCLINICAL PHARMACOLOGICAL CHARACTERIZATION OF THE BACE1 INHIBITOR LY3202626

Authors: 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.

Source: Alzheimer's & dementia. 12(7):P432-P433

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100093207840.0x000001&indx=1&recIds=ETOCvdc_100093207840.0x000001

Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor

Authors: 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.

Source: Journal of Medicinal Chemistry; June 2021, Vol. 64 Issue: 12 p8076-8100, 25p

Preclinical characterization of LY2886721: A BACE1 inhibitor in clinical development for early Alzheimer's disease

Authors: May, Patrick, Boggs, Leonard, Brier, Richard, Calligaro, David, Citron, Martin, Day, Theresa, Lin, Suizhen, Lindstrom, Terry, Mergott, Dustin, Monk, Scott, Sanchez-Felix, Manuel Vicente, Sheehan, Scott, Vaught, Grant, Yang, Zhixiang, Audia, James

Source: Alzheimer's & dementia. 8(4):P704-P705

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100049620221.0x000001&indx=1&recIds=ETOCvdc_100049620221.0x000001

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A CORRELATIONAL ANALYSIS OF EXPOSURE AND PHARMACODYNAMIC EFFECTS OF THE BACE1 INHIBITOR LY3202626 IN PDAPP MICE FOLLOWING ACUTE ORAL DOSING

Authors: 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.

Source: In Alzheimer's & Dementia: The Journal of the Alzheimer's Association July 2016 12(7) Supplement:P831-P831

The Potent BACE1 Inhibitor LY2886721 Elicits Robust Central Aβ Pharmacodynamic Responses in Mice, Dogs, and Humans.

Authors: 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, Celedón R., James, Douglas E., Jhee, Stanford S., Komjathy, Steven F., Li, Linglin

Source: Journal of Neuroscience; 1/21/2015, Vol. 35 Issue 3, p1199-1210, 12p

Subject Terms: PROTEASE inhibitors, AMYLOID beta-protein, ALZHEIMER'S disease, CLINICAL trials, NEURODEGENERATION, MEMORY loss, DEMENTIA

The development of potent and selective bisarylmaleimide GSK3 inhibitors

Authors: Engler, Thomas A. ^⁎, Malhotra, Sushant, Burkholder, Timothy P., Henry, James R., Mendel, David, Porter, Warren J., Furness, Kelly, Diefenbacher, Clive, Marquart, Angela, Reel, Jon K., Li, Yihong, Clayton, Joshua, Cunningham, Brian, McLean, Johnathan, O’Toole, John C., Brozinick, Joseph, Hawkins, Eric, Misener, Elizabeth, Briere, Daniel, Brier, Richard A., Wagner, Jill R., Campbell, Robert M., Anderson, Bryan D., Vaughn, Renee, Bennett, Donald B., Meier, Timothy I., Cook, James A.

Source: In Bioorganic & Medicinal Chemistry Letters 2005 15(4):899-903

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