Zobrazeno 1 - 10
of 33
pro vyhledávání: '"Robert C, Wahl"'
Autor:
Andrew Tasker, Andreas Reichelt, Yi-Ling Hu, Deanna Mohn, John McCarter, Ben Fisher, Robert M. Rzasa, Yi Chen, Julio C. Medina, Gang Yu, Sharon Wannberg, Brian Lucas, Ron C. Kelly, Jennifer Seganish, Felix Gonzalez-Lopez de Turiso, Xiaolin Hao, Kristin L. Andrews, Douglas A. Whittington, Matthew Frank Brown, Dawei Zhang, Youngsook Shin, Mario G. Cardozo, Jason Duquette, Robert C. Wahl, Leeanne Zalameda, Daniela Metz, Vatee Pattaropong, Michael G. Johnson, Tisha San Miguel, Randall W. Hungate, John Whoriskey, Lawrence R. McGee, Timothy D. Cushing, Kirk Henne, Liping H. Pettus, Xiao He
Publikováno v:
Journal of Medicinal Chemistry. 58:480-511
The development and optimization of a series of quinolinylpurines as potent and selective PI3Kδ kinase inhibitors with excellent physicochemical properties are described. This medicinal chemistry effort led to the identification of 1 (AMG319), a com
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::41f464b8458b3d559ce036ed30580e01
https://doi.org/10.1021/jm501624r
https://doi.org/10.1021/jm501624r
Autor:
Paul H. Wen, Robert C. Wahl, Ryan White, Oleg Epstein, Stephen J. Wood, Katayoun Derakhchan, Douglas A. Whittington, Chuck E. Kreiman, Isaac E. Marx, Thomas Dineen, Dean Hickman, Kui Chen, Matthew Weiss, Joel Esmay, Vinod F. Patel, Alan C. Cheng, Robert T. Fremeau
Publikováno v:
Journal of Medicinal Chemistry. 57:9811-9831
We have previously shown that the aminooxazoline xanthene scaffold can generate potent and orally efficacious BACE1 inhibitors although certain of these compounds exhibited potential hERG liabilities. In this article, we describe 4-aza substitution o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c9b3095ff7f5efcf8cbc5e633bdfc8f
https://doi.org/10.1021/jm5012676
https://doi.org/10.1021/jm5012676
Autor:
Kate S, Ashton, Kristin L, Andrews, Marian C, Bryan, Marion C, Bryan, Jie, Chen, Kui, Chen, Michelle, Chen, Samer, Chmait, Michael, Croghan, Rod, Cupples, Christopher, Fotsch, Joan, Helmering, Steve R, Jordan, Robert J M, Kurzeja, Klaus, Michelsen, Lewis D, Pennington, Steve F, Poon, Glenn, Sivits, Gwyneth, Van, Steve L, Vonderfecht, Robert C, Wahl, Jiandong, Zhang, David J, Lloyd, Clarence, Hale, David J, St Jean
Publikováno v:
Journal of Medicinal Chemistry. 57:309-324
Small molecule activators of glucokinase have shown robust efficacy in both preclinical models and humans. However, overactivation of glucokinase (GK) can cause excessive glucose turnover, leading to hypoglycemia. To circumvent this adverse side effe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::688eef24bebd019f68813ef22be87641
https://doi.org/10.1021/jm4016735
https://doi.org/10.1021/jm4016735
Autor:
Kui Chen, Daniel La, Michael D. Bartberger, Russell Graceffa, Thomas T. Nguyen, Tisha San Miguel, E. Allen Sickmier, Ryan Brown, Vivian S. W. Li, Stephen J. Wood, Lewis D. Pennington, James Brown, Jianhua Zhang, Craig E. Masse, Holger Monenschein, Patricia Lopez, Dean Hickman, Brian K. Albrecht, May Xue, Michael Croghan, Scott Harried, Safura Babu-Khan, Yuan Cheng, Yi Luo, Martin Citron, Matthew R. Kaller, Patricia Amarante, Wenge Zhong, Paul H. Wen, Bryant Yang, Robert C. Wahl, Matthew Weiss, Chuck Kriemen, Stephen Hitchcock, Vinod F. Patel, Ted Judd, Toni Williamson
Publikováno v:
ACS Medicinal Chemistry Letters. 3:886-891
β-Secretase inhibitors are potentially disease-modifying treatments for Alzheimer's disease. Previous efforts in our laboratory have resulted in hydroxyethylamine-derived inhibitors such as 1 with low nanomolar potency against β-site amyloid precur
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e1836b589b3ebfe48433f1f6f45d8355
https://doi.org/10.1021/ml3000148
https://doi.org/10.1021/ml3000148
Autor:
Yuan Cheng, Matthew R. Kaller, Steven W. Louie, Martin Citron, Lewis D. Pennington, Daniel S. La, Matthew Weiss, Stephen J. Wood, Wenge Zhong, Michael Croghan, Toni Williamson, Scott Harried, James Brown, Kui Chen, Tisha San Miguel, Ronke Imbeah-Ampiah, Holger Monenschein, Qiufen Xue, Hongbing Huang, Patricia Lopez, Claire Rattan, Thomas Dineen, Daniel B. Horne, E. Allen Sickmier, Dean Hickman, Safura Babu-Khan, Charles Kreiman, Vivian S. W. Li, Paul H. Wen, Michael D. Bartberger, Russell Graceffa, Robert C. Wahl, Thomas T. Nguyen, Bryant Yang, Ted Judd, Joel Esmay, Vinod F. Patel, Stephen Hitchcock
Publikováno v:
Journal of Medicinal Chemistry. 55:9009-9024
A series of potent hydroxyethyl amine (HEA) derived inhibitors of β-site APP cleaving enzyme (BACE1) was optimized to address suboptimal pharmacokinetics and poor CNS partitioning. This work identified a series of benzodioxolane analogues that posse
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::282a471f56ccce495f911c58f29307ea
https://doi.org/10.1021/jm300119p
https://doi.org/10.1021/jm300119p
Autor:
Paul H. Wen, Robert C. Wahl, Michael Croghan, Ronke Imbeah-Ampiah, Paul Acton, Stephen J. Wood, Charles Kreiman, Vivian S. W. Li, Qiufen Xue, Lewis D. Pennington, Safura Babu-Khan, Daniel B. Horne, Thomas Dineen, Wenge Zhong, Scott Harried, Douglas A. Whittington, Dean Hickman, James Brown, Martin Citron, Matthew Weiss, Daniel S. La, Holger Monenschein, Bryant Yang, E. Allen Sickmier, Tisha San Miguel, Robert T. Dunn, Russell Graceffa, Patricia Lopez, Toni Williamson, Hongbing Huang, Yuan Cheng, Kui Chen, Matthew R. Kaller, Michael D. Bartberger, Steven W. Louie, Hugo M. Vargas, Stephen Hitchcock, Thomas T. Nguyen, Vinod F. Patel, Ted Judd, Joel Esmay
Publikováno v:
Journal of Medicinal Chemistry. 55:9025-9044
We have previously shown that hydroxyethylamines can be potent inhibitors of the BACE1 enzyme and that the generation of BACE1 inhibitors with CYP 3A4 inhibitory activities in this scaffold affords compounds (e.g., 1) with sufficient bioavailability
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e8863b7dd3a68852600abaa1a5773f2a
https://doi.org/10.1021/jm300118s
https://doi.org/10.1021/jm300118s
Autor:
Timothy Powers, Stephen J. Wood, Ted Judd, Vivian S. W. Li, James Brown, E. Allen Sickmier, Klaus Michelsen, David J. St. Jean, Yi Luo, Dean Hickman, Yuan Cheng, Kui Chen, Stephen Hitchcock, Steven W. Louie, Patricia Lopez, Brad Jordan, Thomas Nixey, Robert T. Fremeau, Michael D. Bartberger, Paul H. Wen, Robert C. Wahl, Claire Rattan
Publikováno v:
Journal of Medicinal Chemistry. 54:5836-5857
Using fragment-based screening of a focused fragment library, 2-aminoquinoline 1 was identified as an initial hit for BACE1. Further SAR development was supported by X-ray structures of BACE1 cocrystallized with various ligands and molecular modeling
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd6f6e1fa9855cbd5de616743bac67e1
https://doi.org/10.1021/jm200544q
https://doi.org/10.1021/jm200544q
Autor:
Kui Chen, Ryan White, Robert T. Fremeau, Stephen J. Wood, Oleg Epstein, Scott Harried, Paul H. Wen, Michael D. Bartberger, James Brown, Robert C. Wahl, Douglas A. Whittington, Robert T. Dunn, Xiao Mei Zheng, Matthew Weiss, Yuan Cheng, Patricia Lopez, Dean Hickman, Wenyuan Qian, Jian J. Chen, Vinod F. Patel, Timothy Powers, Ted Judd, Yi Luo, Ana Elena Minatti, Stephen Hitchcock, Hugo M. Vargas
BACE1 inhibition to prevent Aβ peptide formation is considered to be a potential route to a disease-modifying treatment for Alzheimer’s disease. Previous efforts in our laboratory using a combined structure- and property-based approach have result
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0e2bfa91afe6b471a946b0ea848dad64
https://europepmc.org/articles/PMC4329588/
https://europepmc.org/articles/PMC4329588/
Autor:
Wen Zhou, Murray O. Robinson, Hue Kha, Robert C. Wahl, Brian Rasnow, Karen Kearns, Tisha San Miguel, Alex Mladenovic, Barbara Karan-Tamir, Lisa Zeni, Kui Chen
Publikováno v:
Analytical Biochemistry. 331:230-234
A telomerase assay has been developed for high-throughput screening in 96-well microtiter plates. A crude cell lysate which adds telomere repeats to a biotinylated DNA primer is the source of telomerase. The telomerase-extended primer is hybridized t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee4936ab7b4262b099fa7c1bc3e3e1c1
https://doi.org/10.1016/j.ab.2004.03.073
https://doi.org/10.1016/j.ab.2004.03.073
Autor:
Paul H. Wen, Robert C. Wahl, Ryan White, Zihao Hua, Robert T. Fremeau, Thomas Dineen, Stephen J. Wood, Jason Brooks Human, Vinod F. Patel, Marian C. Bryan, Oleg Epstein, Douglas A. Whittington, Katayoun Derakhchan, Charles Kreiman, Matthew Weiss, Alan C. Cheng, Dean Hickman, Xiao Mei Zheng, Isaac E. Marx
Publikováno v:
Journal of medicinal chemistry. 57(23)
The optimization of a series of aminooxazoline xanthene inhibitors of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) is described. An early lead compound showed robust Aβ lowering activity in a rat pharmacodynamic model, but advancement
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e24e5ad84e0c301aadb1173bf80a9f3
https://pubmed.ncbi.nlm.nih.gov/25389560
https://pubmed.ncbi.nlm.nih.gov/25389560