Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Stephanie L. Stout"'
Autor:
Kristy Kikly, Howard Barff Broughton, William Chang, Selma Sapmaz, Richard Morphy, Holly A. Bina, Jim D. Durbin, Sherry Y Guo, Timothy Ivo Richardson, Jimmy P Steele, Ryan Edward Stites, Brian G. Getman, Vaught Grant Matthews, Veavi Ching-Yun Chang, Pamela K. Shetler, Greg L Durst, Denise D Edmondson, Rob Barr, Helene Rudyk, Charles Willis Lugar, Nita J. Patel, Christian Alexander Clarke, Kelly Wayne Furness, Nicole E New, David K. Clawson, Keith R. Stayrook, Mark Chambers, Brian Michael Mathes, Stephanie L. Stout, Wendy H. Gough
Publikováno v:
Journal of Medicinal Chemistry. 64:5470-5484
The Th17 pathway has been implicated in autoimmune diseases. The retinoic acid receptor-related orphan receptor C2 (RORγt) is a master regulator of Th17 cells and controls the expression of IL-17A. RORγt is expressed primarily in IL-17A-producing l
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
Autor:
Charles W, Lugar, Christian A, Clarke, Richard, Morphy, Helene, Rudyk, Selma, Sapmaz, Ryan E, Stites, Grant M, Vaught, Kelly, Furness, Howard B, Broughton, Greg L, Durst, David K, Clawson, Stephanie L, Stout, Sherry Y, Guo, Jim D, Durbin, Keith R, Stayrook, Denise D, Edmondson, Kristy, Kikly, Nicole E, New, Holly A, Bina, Mark G, Chambers, Pamela, Shetler, William Y, Chang, Veavi Ching-Yun, Chang, Rob, Barr, Wendy H, Gough, Jimmy P, Steele, Brian, Getman, Nita, Patel, Brian M, Mathes, Timothy I, Richardson
Publikováno v:
Journal of medicinal chemistry. 64(9)
The Th17 pathway has been implicated in autoimmune diseases. The retinoic acid receptor-related orphan receptor C2 (RORγt) is a master regulator of Th17 cells and controls the expression of IL-17A. RORγt is expressed primarily in IL-17A-producing l
Autor:
Philip J. Ebert, Gary L. Heady, Bruce W. Konicek, Melinda D. Willard, Stephanie L. Stout, Julie Stewart, David E. Timm, Yi Zeng, Victoria L. Peek, Suzane L. Um, Isabella H. Wulur, Beverly L. Falcon, Andrew Capen, Kelly M. Credille, Yong Wang, Jennifer R. Stephens, Sau-Chi Betty Yan, Richard A. Walgren, Bharvin K. R. Patel
Publikováno v:
Oncotarget
Merestinib is an oral multi-kinase inhibitor targeting a limited number of oncokinases including MET, AXL, RON and MKNK1/2. Here, we report that merestinib inhibits neurotrophic receptor tyrosine kinases NTRK1/2/3 which are oncogenic drivers in tumor
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
Autor:
Mark Edward Rempala, Tom Raub, Carlos Mateos, Sehila Pleite, Josh Clayton, William J. Ehlhardt, Huaxing Pei, Bradley Condon, Stephanie L. Stout, Sheela Ashok, Sandaruwan Geeganage, Mei Lai, Burkholder Timothy P, Deidre Michelle Johns, Yong Wang, Kenneth James Junior Henry, Saravanan Parthasarathy, Zhohai Lu, Oscar de Frutos, Pablo A. García
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(10)
During the course of our research efforts to develop potent and selective AKT inhibitors, we discovered enatiomerically pure substituted dihydropyridopyrimidinones (DHP) as potent inhibitors of protein kinase B/AKT with excellent selectivity against
Autor:
Thierry Masquelin, Gary G. Deng, Prabhakar Kondaji Jadhav, Balagopalakrishna Chavali, David E. Timm, Najia Jin, Stephanie L. Stout, Mark J. Nilges, William F. Matter
Publikováno v:
Applied Magnetic Resonance
As an early visitor to the injured loci, neutrophil-derived human Myeloperoxidase (hMPO) offers an attractive protein target to modulate the inflammation of the host tissue through suitable inhibitors. We describe a novel methodology of using low tem
Autor:
C. Lin, Chin Liu, Valentine J. Klimkowski, Craig A. Swearingen, Lisa A. Adams, Stephanie L. Stout, Timothy B. Durham, Michael Robert Wiley, Kannan Thirunavukkarasu, Mark Chambers, Jim D. Durbin, Christopher John Rito, Jothirajah Marimuthu, James Lee Toth
Publikováno v:
Journal of Medicinal Chemistry. 57:10476-10485
A disintegrin and metalloproteinase with thrombospondin motifs-4 (ADAMTS-4) and ADAMTS-5 are zinc metalloproteases commonly referred to as aggrecanase-1 and aggrecanase-2, respectively. These enzymes are involved in the degradation of aggrecan, a key
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
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/