Synthesis of pyrimido[4,5-c]azepine- and pyrimido[4,5-c]oxepine-based γ-secretase modulators von Wu, Yong-Jin, Zhang, Yunhui, Toyn, Jeremy H., Macor, John E., Thompson, Lorin A.

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The γ-Secretase Modulator, BMS-932481, Modulates Aβ Peptides in the Plasma and Cerebrospinal Fluid of Healthy Volunteers von Soares, Holly D, Gasior, Maciej, Toyn, Jeremy H, Wang, Jun-Sheng, Hong, Quan, Berisha, Flora, Furlong, Michael T, Raybon, Joseph, Lentz, Kimberley A, Sweeney, Francis, Zheng, Naiyu, Akinsanya, Billy, Berman, Robert M, Thompson, Lorin A, Olson, Richard E, Morrison, John, Drexler, Dieter M, Macor, John E, Albright, Charlie F, Ahlijanian, Michael K, AbuTarif, Malaz

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Synthesis of functionalized derivatives of the gamma-secretase modulator BMS-932481 and identification of its major metabolite von Zhang, Yunhui, Boy, Kenneth M., Wu, Yong-Jin, Ramirez, Antonio, Toyn, Jeremy H., Ahlijanian, Michael K., Albright, Charles F., Zhuo, Xiaoliang, Johnson, Benjamin M., Denton, R. Rex, Olson, Richard E., Thompson, Lorin A., Macor, John E.

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Viable mouse gene ablations that robustly alter brain Aβ levels are rare von Toyn, Jeremy H, Lin, Xu-Alan, Thompson, Mark W, Guss, Valerie, Meredith, Jr, Jere E, Sankaranarayanan, Sethu, Barrezueta, Nestor, Corradi, John, Majumdar, Antara, Small, Daniel L, Hansard, Melissa, Lanthorn, Thomas, Westphal, Ryan S, Albright, Charles F

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γ-Secretase Pharmacology : What Pharmacology Will Work for Alzheimer's Disease? von Toyn, Jeremy H., Rowley, Adele, Matsuoka, Yasuji, Tomita, Taisuke, Imbimbo, Bruno P.

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Discovery of S3-Truncated, C‑6 Heteroaryl Substituted Aminothiazine β‑Site APP Cleaving Enzyme‑1 (BACE1) Inhibitors von Wu, Yong-Jin, Guernon, Jason, Shi, Jianliang, Marcin, Lawrence, Higgins, Mendi, Rajamani, Ramkumar, Muckelbauer, Jodi, Lewis, Hal, Chang, ChiehYing, Camac, Dan, Toyn, Jeremy H, Ahlijanian, Michael K, Albright, Charles F, Macor, John E, Thompson, Lorin A

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Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors von Wu, Yong-Jin, Guernon, Jason, Rajamani, Ramkumar, Toyn, Jeremy H., Ahlijanian, Michael K., Albright, Charles F., Muckelbauer, Jodi, Chang, ChiehYing, Camac, Dan, Macor, John E., Thompson, Lorin A.

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Pharmacodynamics of selective inhibition of γ-secretase by avagacestat von Albright, Charles F, Dockens, Randy C, Meredith, Jr, Jere E, Olson, Richard E, Slemmon, Randy, Lentz, Kimberley A, Wang, Jun-Sheng, Denton, R Rex, Pilcher, Gary, Rhyne, Paul W, Raybon, Joseph J, Barten, Donna M, Burton, Catherine, Toyn, Jeremy H, Sankaranarayanan, Sethu, Polson, Craig, Guss, Valerie, White, Randy, Simutis, Frank, Sanderson, Thomas, Gillman, Kevin W, Starrett, Jr, John E, Bronson, Joanne, Sverdlov, Oleksandr, Huang, Shu-Pang, Castaneda, Lorna, Feldman, Howard, Coric, Vlad, Zaczek, Robert, Macor, John E, Houston, John, Berman, Robert M, Tong, Gary

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Interpreting Alzheimer's disease clinical trials in light of the effects on amyloid-β von Toyn, Jeremy H, Ahlijanian, Michael K

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Robust Translation of γ-Secretase Modulator Pharmacology across Preclinical Species and Human Subjects von Toyn, Jeremy H, Boy, Kenneth M, Raybon, Joseph, Meredith, Jr, Jere E, Robertson, Alan S, Guss, Valerie, Hoque, Nina, Sweeney, Francis, Zhuo, Xiaoliang, Clarke, Wendy, Snow, Kimberly, Denton, R Rex, Zuev, Dmitry, Thompson, Lorin A, Morrison, John, Grace, James, Berisha, Flora, Furlong, Michael, Wang, Jun-Sheng, Lentz, Kimberly A, Padmanabha, Ramesh, Cook, Lynda, Wei, Cong, Drexler, Dieter M, Macor, John E, Albright, Charlie F, Gasior, Maciej, Olson, Richard E, Hong, Quan, Soares, Holly D, AbuTarif, Malaz, Ahlijanian, Michael K

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Synergistic inhibition of Aβ production by combinations of γ-secretase modulators von Robertson, Alan S., Iben, Lawrence G., Wei, Cong, Meredith, Jere E., Drexler, Dieter M., Banks, Martyn, Vite, Gregory D., Olson, Richard E., Thompson, Lorin A., Albright, Charles F., Ahlijanian, Michael K., Toyn, Jeremy H.

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Acyl Guanidine Inhibitors of β‑Secretase (BACE-1): Optimization of a Micromolar Hit to a Nanomolar Lead via Iterative Solid- and Solution-Phase Library Synthesis von Gerritz, Samuel W, Zhai, Weixu, Shi, Shuhao, Zhu, Shirong, Toyn, Jeremy H, Meredith, Jere E, Iben, Lawrence G, Burton, Catherine R, Albright, Charles F, Good, Andrew C, Tebben, Andrew J, Muckelbauer, Jodi K, Camac, Daniel M, Metzler, William, Cook, Lynda S, Padmanabha, Ramesh, Lentz, Kimberley A, Sofia, Michael J, Poss, Michael A, Macor, John E, Thompson, Lorin A

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Design and optimization of tricyclic gamma-secretase modulators von Shi, Jianliang, Zuev, Dmitry, Xu, Li, Lentz, Kimberley A., Grace, James E., Toyn, Jeremy H., Olson, Richard E., Macor, John E., Thompson, Lorin A.

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Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor von Gillman, Kevin W, Starrett, John E, Parker, Michael F, Xie, Kai, Bronson, Joanne J, Marcin, Lawrence R, McElhone, Kate E, Bergstrom, Carl P, Mate, Robert A, Williams, Richard, Meredith, Jere E, Burton, Catherine R, Barten, Donna M, Toyn, Jeremy H, Roberts, Susan B, Lentz, Kimberley A, Houston, John G, Zaczek, Robert, Albright, Charles F, Decicco, Carl P, Macor, John E, Olson, Richard E

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Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aβ Reduction in Rodents von Wu, Yong-Jin, Guernon, Jason, Yang, Fukang, Snyder, Lawrence, Shi, Jianliang, Mcclure, Andrea, Rajamani, Ramkumar, Park, Hyunsoo, Ng, Alicia, Lewis, Hal, Chang, ChiehYing, Camac, Dan, Toyn, Jeremy H, Ahlijanian, Michael K, Albright, Charles F, Macor, John E, Thompson, Lorin A

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The Swi5 transcription factor of Saccharomyces cerevisiae has a role in exit from mitosis through induction of the cdk-inhibitor Sic1 in telophase von Toyn, J.H. (National Institute for Medical Research, London, UK.), Johnson, A.L, Donovan, J.D, Toone, W.M, Johnston, L.H

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Macrocyclic prolinyl acyl guanidines as inhibitors of β-secretase (BACE) von Boy, Kenneth M., Guernon, Jason M., Wu, Yong-Jin, Zhang, Yunhui, Shi, Joe, Zhai, Weixu, Zhu, Shirong, Gerritz, Samuel W., Toyn, Jeremy H., Meredith, Jere E., Barten, Donna M., Burton, Catherine R., Albright, Charles F., Good, Andrew C., Grace, James E., Lentz, Kimberley A., Olson, Richard E., Macor, John E., Thompson, Lorin A.

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Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ‑Secretase Modulator BMS-932481 von Boy, Kenneth M, Guernon, Jason M, Zuev, Dmitry S, Xu, Li, Zhang, Yunhui, Shi, Jianliang, Marcin, Lawrence R, Higgins, Mendi A, Wu, Yong-Jin, Krishnananthan, Subramaniam, Li, Jianqing, Trehan, Ashok, Smith, Daniel, Toyn, Jeremy H, Meredith, Jere E, Burton, Catherine R, Kimura, S. Roy, Zvyaga, Tatyana, Zhuo, Xiaoliang, Lentz, Kimberley A, Grace, James E, Denton, Rex, Morrison, John S, Mathur, Arvind, Albright, Charles F, Ahlijanian, Michael K, Olson, Richard E, Thompson, Lorin A, Macor, John E

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The Amyloid-β Rise and γ-Secretase Inhibitor Potency Depend on the Level of Substrate Expression von Burton, Catherine R., Meredith, Jere E., Barten, Donna M., Goldstein, Margi E., Krause, Carol M., Kieras, Cathy J., Sisk, Lisa, Iben, Lawrence G., Polson, Craig, Thompson, Mark W., Lin, Xu-Alan, Corsa, Jason, Fiedler, Tracey, Pierdomenico, Maria, Cao, Yang, Roach, Arthur H., Cantone, Joseph L., Ford, Michael J., Drexler, Dieter M., Olson, Richard E., Yang, Michael G., Bergstrom, Carl P., McElhone, Kate E., Bronson, Joanne J., Macor, John E., Blat, Yuval, Grafstrom, Robert H., Stern, Andrew M., Seiffert, Dietmar A., Zaczek, Robert, Albright, Charles F., Toyn, Jeremy H.

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Swi5 controls a novel wave of cyclin synthesis in late mitosis von Aerne, B L, Johnson, A L, Toyn, J H, Johnston, L H

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