Zobrazeno 1 - 10
of 57
pro vyhledávání: '"Charles E, Nolan"'
Autor:
Andrea M. Zuhl, Charles E. Nolan, Michael A. Brodney, Sherry Niessen, Kevin Atchison, Christopher Houle, David A. Karanian, Claude Ambroise, Jeffrey W. Brulet, Elizabeth M. Beck, Shawn D. Doran, Brian T. O’Neill, Christopher W. am Ende, Cheng Chang, Kieran F. Geoghegan, Graham M. West, Joshua C. Judkins, Xinjun Hou, David R. Riddell, Douglas S. Johnson
Publikováno v:
Nature Communications, Vol 7, Iss 1, Pp 1-14 (2016)
Several β-secretase (BACE) inhibitors exhibit unexplained ocular toxicity in preclinical studies. Here the authors generate a clickable photoaffinity probe to interrogate off-targets in cells and animals, and identify inhibition of cathepsin D as a
Externí odkaz:
https://doaj.org/article/5dfe4a29e6af43a49ee6c24207abc513
Autor:
Laigao Chen, Anabella Villalobos, Ryosuke Arakawa, Shawn D. Doran, Christer Halldin, Brian T. O’Neill, Akihiro Takano, Michael Aaron Brodney, Nahid Amini, Charles E. Nolan, Timothy J. McCarthy, Jason K. Dutra, Sangram Nag, Cheng Chang, Lei Zhang
Publikováno v:
Journal of Nuclear Medicine. 60:992-997
Beta-secretase 1 (BACE1) is a key enzyme in the generation of beta-amyloid, which is accumulated in the brain of Alzheimer’s disease (AD) patients. PF-06684511 was identified as a candidate PET ligand for imaging BACE1 in the brain, and showed high
Autor:
Kelly R. Bales, Anabella Villalobos, David Riddell, Shawn D. Doran, Christopher Ryan Butler, Bruce N. Rogers, Lorraine F. Lanyon, Karamjeet Pandher, Claude Ambroise, Ashley Robshaw, Gabriela Barreiro, Christopher Houle, Kevin Ogilvie, Brian T. O’Neill, Erik Alphie Lachapelle, Germaine Boucher, Xinjun Hou, Katherine Hales, David Karanian, Michael Aaron Brodney, Leanne M. Buzon, Kimberly Lapham, Lei Zhang, Luis Martinez-Alsina, Charles E. Nolan, Claire M. Steppan, Cathleen Gonzales, John C. Murray, Cheng Chang, Jason K. Dutra, Elizabeth Mary Beck
Publikováno v:
Journal of Medicinal Chemistry. 61:4476-4504
A major challenge in the development of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors for the treatment of Alzheimer's disease is the alignment of potency, drug-like properties, and selectivity over related aspartyl proteases
Autor:
Felix Vajdos, Eric Benvenuti, Leanne M. Buzon, Brian T. O’Neill, Gabriela Barreiro, David Riddell, Kevin Atchison, Charles E. Nolan, Ashley Robshaw, Eric F. Johnson, Kevin D. Parris, Shawn D. Doran, Michael Aaron Brodney, Xinjun Hou, Luis Martinez-Alsina, Kimberly Lapham, Mei-Hui Hsu, Elizabeth Mary Beck, Christopher Ryan Butler, Kevin Ogilvie, Cathleen Gonzales, Lorraine F. Lanyon, Christopher John Helal
Publikováno v:
Journal of Medicinal Chemistry
A growing subset of β-secretase (BACE1) inhibitors for the treatment of Alzheimer's disease (AD) utilizes an anilide chemotype that engages a key residue (Gly230) in the BACE1 binding site. Although the anilide moiety affords excellent potency, it s
Autor:
Akihiro, Takano, Laigao, Chen, Sangram, Nag, Michael A, Brodney, Ryosuke, Arakawa, Cheng, Chang, Nahid, Amini, Shawn D, Doran, Jason K, Dutra, Timothy J, McCarthy, Charles E, Nolan, Brian T, O'Neill, Anabella, Villalobos, Lei, Zhang, Christer, Halldin
Publikováno v:
Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 60(7)
β-secretase 1 (BACE1) is a key enzyme in the generation of β-amyloid, which is accumulated in the brain of Alzheimer disease patients. PF-06684511 was identified as a candidate PET ligand for imaging BACE1 in the brain and showed high specific bind
Autor:
Charles E. Nolan, Christer Halldin, Anabella Villalobos, Kelly R. Bales, Klaas Schildknegt, Ryosuke Arakawa, Akihiro Takano, Lorraine F. Lanyon, Leanne M. Buzon, Shawn D. Doran, Nahid Amini, Laigao Chen, Brian T. O’Neill, Michael Aaron Brodney, Elizabeth Mary Beck, Lei Zhang, Timothy J. McCarthy, Sangram Nag, Jason K. Dutra
Publikováno v:
Journal of medicinal chemistry. 61(8)
Alzheimer’s disease (AD) is characterized by accumulation of β-amyloid (Aβ) plaques and neurofibrillary tau tangles in the brain. β-Site amyloid precursor protein cleaving enzyme 1 (BACE1) plays a key role in the generation of Aβ fragments via
Autor:
Christopher John Helal, Kevin Atchison, Christopher Ryan Butler, Cathleen Gonzales, Ricardo Lira, Shawn D. Doran, Feng Pan, Felix Vajdos, Alison H. Varghese, Gabriela Barreiro, Michael Aaron Brodney, Jinlong Wang, Elizabeth Mary Beck, Luis Martinez-Alsina, Yong Zhang, Kevin D. Parris, David Riddell, Joseph Michael Young, Leanne M. Buzon, Ashley Robshaw, Kevin Ogilvie, Jason K. Dutra, Brian T. O’Neill, John C. Murray, Charles E. Nolan
Publikováno v:
Journal of Medicinal Chemistry. 58:2678-2702
The identification of centrally efficacious β-secretase (BACE1) inhibitors for the treatment of Alzheimer's disease (AD) has historically been thwarted by an inability to maintain alignment of potency, brain availability, and desired absorption, dis
Autor:
Mark W. Bundesmann, David Riddell, Peter Mikochik, Leanne M. Buzon, Brian T. O’Neill, Subas M. Sakya, Jayvardhan Pandit, Christopher Ryan Butler, Xinjun Hou, Ashley Robshaw, Kevin D. Parris, Jason K. Dutra, Ricardo Lira, Loren M. Price, Charles E. Nolan, Elizabeth Mary Beck, Bruce N. Rogers, Gabriela Barreiro, Aijia Yu, Michael Aaron Brodney, Cathleen Gonzales, Erik Alphie Lachapelle, Shawn D. Doran, Luis Martinez-Alsina, Kevin E. Henegar, Ying Fan, Kevin Atchison, Eric F. Johnson, John C. Murray, Kevin Ogilvie, Yong Zhang
Publikováno v:
Journal of Medicinal Chemistry
In recent years, the first generation of β-secretase (BACE1) inhibitors advanced into clinical development for the treatment of Alzheimer’s disease (AD). However, the alignment of drug-like properties and selectivity remains a major challenge. Her
Autor:
Jeffrey W Brulet, Christopher W. am Ende, Michael Aaron Brodney, Sherry Niessen, Brian T. O’Neill, Kevin Atchison, Douglas S. Johnson, Kieran F. Geoghegan, David Riddell, Charles E. Nolan, Elizabeth Mary Beck, Graham M. West, David Karanian, Cheng Chang, Shawn D. Doran, Xinjun Hou, Christopher Houle, Andrea M. Zuhl, Claude Ambroise, Joshua C. Judkins
Publikováno v:
Nature Communications, Vol 7, Iss 1, Pp 1-14 (2016)
Nature Communications
Nature Communications
Inhibition of β-secretase BACE1 is considered one of the most promising approaches for treating Alzheimer's disease. Several structurally distinct BACE1 inhibitors have been withdrawn from development after inducing ocular toxicity in animal models,
Autor:
Kelly R. Bales, David Karanian, Michael Aaron Brodney, Shawn D. Doran, Cathleen Gonzales, Katherine Hales, Germaine Boucher, Lorraine F. Lanyon, Charles E. Nolan, Karamjeet Pandher, Christopher Houle, Claude Ambroise, Cheng Chang
Publikováno v:
Alzheimer's & Dementia. 12