Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Richard A. Brier"'
Autor:
Brian A. Willis, Stephen L. Lowe, Scott A. Monk, Patrick J. Cocke, Christopher D. Aluise, Leonard N. Boggs, Anthony R. Borders, Richard A. Brier, Robert A. Dean, Steven J. Green, Douglas E. James, Stanford S. Jhee, Qun Lin, Albert C. Lo, Patrick C. May, Brian M. Watson, Leonard L. Winneroski, Zhixiang Yang, Jennifer A. Zimmer, David L. McKinzie, Dustin J. Mergott
Publikováno v:
Journal of Alzheimer's disease reports. 6(1)
Background: The development of beta-site amyloid-beta precursor protein cleaving enzyme (BACE) 1 inhibitors for the treatment of Alzheimer’s disease requires optimization of inhibitor potency, selectivity, and brain penetration. Moreover, there is
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::912368ce5d97e52cb749b71026a53952
https://pubmed.ncbi.nlm.nih.gov/35243208
https://pubmed.ncbi.nlm.nih.gov/35243208
Autor:
Stephanie L. Stout, Leonard L. Winneroski, Jorg Hendle, Warren J. Porter, Patrick J. C. May, Leonard N. Boggs, Thomas K. Baker, James P. Beck, Steven James Green, Anthony R. Borders, Erik James Hembre, Stephen L. Lowe, Christopher D Aluise, David L. McKinzie, Brian Morgan Watson, Brian Michael Mathes, Jon A. Erickson, Zhixiang Yang, Patrick J Cocke, Dustin J. Mergott, Brian A. Willis, Scott A. Monk, Pablo Garcia-Losada, David E. Timm, Richard A. Brier, Jose Eduardo Lopez
Publikováno v:
Journal of medicinal chemistry. 64(12)
The beta-site APP cleaving enzyme 1, known as BACE1, has been a widely pursued Alzheimer's disease drug target owing to its critical role in the production of amyloid-beta. We have previously reported the clinical development of LY2811376 and LY28867
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::698057ee408d2f35c662510d099e51b3
https://pubmed.ncbi.nlm.nih.gov/34081466
https://pubmed.ncbi.nlm.nih.gov/34081466
Autor:
David E. Timm, Leonard N. Boggs, Brian Michael Mathes, Yuan Shi, Mario Barberis, Zhixiang Yang, Dustin J. Mergott, Scott A. Monk, Pablo Garcia-Losada, Jose Miguel Minguez, Leonard L. Winneroski, Jon A. Erickson, Richard A. Brier, Anthony R. Borders, Stephanie L. Stout, Porter Warren J, Zoran Rankovic, Jose Eduardo Lopez, Erik James Hembre, James E. Audia, Jorg Hendle, James P. Beck, Steven James Green, Brian Morgan Watson, Patrick C. May, Robert D. Boyer
Publikováno v:
Bioorganic & Medicinal Chemistry. 28:115194
Inhibition of BACE1 has become an important strategy in the quest for disease modifying agents to slow the progression of Alzheimer's disease. We previously reported the fragment-based discovery of LY2811376, the first BACE1 inhibitor reported to dem
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::686975880a947f8f81325a11d876e66b
https://doi.org/10.1016/j.bmc.2019.115194
https://doi.org/10.1016/j.bmc.2019.115194
Autor:
Bruce W. Shaw, Yuke Zhang, Kenneth C. Cassidy, Robert M. Christie, Prabhakar Kondaji Jadhav, Jim D. Durbin, Gary G. Deng, Matthew Allen Schiffler, Kostas Gavardinas, Richard A. Brier, Keyun Qing, Donald P. Matthews, Michael A. Staszak, William F. Matter, Yong Wang, Kim Euibong Jemes, D. Scott Coffey
Publikováno v:
ACS Medicinal Chemistry Letters. 5:1138-1142
Cathepsin S (Cat S) plays an important role in many pathological conditions, including abdominal aortic aneurysm (AAA). Inhibition of Cat S may provide a new treatment for AAA. To date, several classes of Cat S inhibitors have been reported, many of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6393a9fc5f96e20e55b6bf40e534a7b3
https://doi.org/10.1021/ml500283g
https://doi.org/10.1021/ml500283g
Autor:
Patrick C. May, Richard A. Brier, Leonard N. Boggs, David L. McKinzie, Leonard L. Winneroski, Anthony R. Borders, Steven James Green, Zhixiang Yang, Dustin J. Mergott, Scott A. Monk
Publikováno v:
Alzheimer's & Dementia. 12
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bb3fe393c7ae5674f4f9d6f9c640bd63
https://doi.org/10.1016/j.jalz.2016.06.1693
https://doi.org/10.1016/j.jalz.2016.06.1693
Autor:
Brian A. Willis, Zhixiang Yang, Dustin J. Mergott, Scott A. Monk, Richard A. Brier, Anthony R. Borders, Patrick J. C. May, Steven James Green, David L. McKinzie, Leonard L. Winneroski, Leonard N. Boggs
Publikováno v:
Alzheimer's & Dementia. 12
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ce9117800559ea83b6343abfc6cabbe1
https://doi.org/10.1016/j.jalz.2016.06.828
https://doi.org/10.1016/j.jalz.2016.06.828
Autor:
Stephanie L. Stout, Patrick C. May, Brian Morgan Watson, Pablo Garcia Losada, Valentine J. Klimkowski, Brian Michael Mathes, David E. Timm, Dustin J. Mergott, Scott A. Monk, Leonard L. Winneroski, Leonard N. Boggs, James P. Beck, James E. Audia, Matthew Allen Schiffler, Richard A. Brier, Anthony R. Borders, Jon A. Erickson, Robert D. Boyer, Kevin John Hudziak
Publikováno v:
Bioorganicmedicinal chemistry. 23(13)
The BACE1 enzyme is a key target for Alzheimer’s disease. During our BACE1 research efforts, fragment screening revealed that bicyclic thiazine 3 had low millimolar activity against BACE1. Analysis of the co-crystal structure of 3 suggested that po
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::01477228c3c9d6ec449c18a60008a90e
https://pubmed.ncbi.nlm.nih.gov/26001341
https://pubmed.ncbi.nlm.nih.gov/26001341
Autor:
Brian Michael Mathes, Zhixiang Yang, Dustin J. Mergott, Scott A. Monk, Hykop Gevorkyan, Larry Ereshefsky, Vaught Grant Matthews, Leonard L. Winneroski, Jon A. Erickson, Stephen L. Lowe, Celedon Gonzales, Scott Martin Sheehan, David E. Timm, Brian Morgan Watson, Ferenc Martenyi, David O. Calligaro, Stephanie L. Stout, Theresa A. Day, Richard A. Brier, Patrick J Cocke, Brian A. Willis, Stanford Jhee, Leonard N. Boggs, Robert A. Dean, James E. Audia, Steven F. Komjathy, Anthony R. Borders, Terry D. Lindstrom, Patrick C. May, Douglas E. James, Linglin Li
BACE1 is a key protease controlling the formation of amyloid β, a peptide hypothesized to play a significant role in the pathogenesis of Alzheimer's disease (AD). Therefore, the development of potent and selective inhibitors of BACE1 has been a focu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f78c69adc5fae76e66024d7197aeccfc
https://europepmc.org/articles/PMC6605527/
https://europepmc.org/articles/PMC6605527/
Autor:
Donald B. Bennett, Brian Eugene Cunningham, Jill R. Wagner, Burkholder Timothy P, O'toole John Cunningham, Daniel A. Briere, David Mendel, Kelly Wayne Furness, Thomas A. Engler, Eric D. Hawkins, Jon K. Reel, Joseph T. Brozinick, Henry James Robert, Renee Vaughn, Robert M. Campbell, Joshua Ryan Clayton, Mclean Johnathan Alexander, Clive Gideon Diefenbacher, Timothy I. Meier, Richard A. Brier, Angela Lynn Marquart, Bryan D. Anderson, James A. Cook, Warren J. Porter, Yihong Li, Elizabeth A. Misener, Sushant Malhotra
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:899-903
Many 3-aryl-4-(1,2,3,4-tetrahydro[1,4]diazepino[6,7,1-hi]indol-7-yl)maleimides exhibit potent GSK3 inhibitory activity (100 nM IC(50)), although few show significant selectivity (100x) versus CDK2, CDK4, or PKCbetaII. However, combining 3-(imidazo[1,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a386c90f11d8bbe8af6add872ac1ee74
https://doi.org/10.1016/j.bmcl.2004.12.063
https://doi.org/10.1016/j.bmcl.2004.12.063
Autor:
Manuel Vicente Sanchez-Felix, Patrick C. May, David O. Calligaro, James E. Audia, Suizhen Lin, Leonard N. Boggs, Zhixiang Yang, Dustin J. Mergott, Scott A. Monk, Theresa A. Day, Richard A. Brier, Vaught Grant Matthews, Terry D. Lindstrom, Martin Citron, Scott Martin Sheehan
Publikováno v:
Alzheimer's & Dementia. 8
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::82c63d71ff40338f2f9dab0af057300e
https://doi.org/10.1016/j.jalz.2012.05.235
https://doi.org/10.1016/j.jalz.2012.05.235