Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Elizabeth F. Brigham"'
Autor:
Daniel Ness, Zhao Ren, Shyra Gardai, Douglas Sharpnack, Victor J Johnson, Richard J Brennan, Elizabeth F Brigham, Andrew J Olaharski
Publikováno v:
PLoS ONE, Vol 8, Iss 6, p e66164 (2013)
Genetic evidence links mutations in the LRRK2 gene with an increased risk of Parkinson's disease, for which no neuroprotective or neurorestorative therapies currently exist. While the role of LRRK2 in normal cellular function has yet to be fully desc
Externí odkaz:
https://doaj.org/article/0e92e327929b407982215728de1da048
Autor:
Susan H. Fox, Jonathon D. S. Holt, Patrick A. Howson, Elizabeth F. Brigham, Tom H. Johnston, Jack T. Nguyen, Michael Hill, Carl Brown, Jonathan M. Brotchie
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 367:373-381
Dyskinesia is a common motor complication associated with the use of levodopa to treat Parkinson's disease. Numerous animal studies in mice, rats, and nonhuman primates have demonstrated that the N-methyl-d-aspartate antagonist, amantadine, dose depe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2206803db7d0f8600b8e41da22d5b52d
https://doi.org/10.1124/jpet.118.247650
https://doi.org/10.1124/jpet.118.247650
Autor:
Anna Liao, Gary Probst, Pamela S. Keim, Kang Hu, Roy K. Hom, David A. Quincy, Michael S. Dappen, Grace T. Kwong, Jenifer Smith, Martin L. Neitzel, Ying-zi Xu, Elizabeth F. Brigham, Kevin P. Quinn, Frédérique Bard, Minghua Sun, Jing Wu, John-Michael Sauer, Dora Kholodenko, Hongbin Zhang, William Wallace, Matthew N. Mattson, Patricia Sacayon, Jacek Jagodzinski, Hing L. Sham, Brian T. Peterson, Simeon Bowers, Jennifer Marugg, Guriqbal S. Basi, Lee H. Latimer, Susanna S. Hemphill, Darren B. Dressen, Karina Wong, Kevin Tanaka, Michael P. Bova, Pamela Santiago, Daniel K. Ness, Anh P. Truong, Wes Zmolek, Lany Ruslim, Christopher Willits, Michael K. Lee, Andrei W. Konradi, Xiaocong M. Ye, Lam Nguyen, Chris M. Semko, Ted A. Yednock, Ruth N. Motter, Albert W. Garofalo, Erich Goldbach, Pearl Tanaka, Danielle L. Aubele
Publikováno v:
Journal of Medicinal Chemistry. 56:5261-5274
Herein, we describe our strategy to design metabolically stable γ-secretase inhibitors which are selective for inhibition of Aβ generation over Notch. We highlight our synthetic strategy to incorporate diversity and chirality. Compounds 30 (ELND006
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c5b61686f688dd0abd9c5edac66d7201
https://doi.org/10.1021/jm301741t
https://doi.org/10.1021/jm301741t
Autor:
Kevin P. Quinn, Marc Adler, Gary Probst, Albert W. Garofalo, Anh P. Truong, Danny Tam, Erich Goldbach, Danielle L. Aubele, Maurizio Franzini, David Chian, Grace Kwong, Xiaocong M. Ye, Zhao Ren, Hing L. Sham, Lany Ruslim, Pearl Tanaka, Elizabeth F. Brigham, Ruth Motter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1974-1977
Mutations in leucine-rich repeat kinase 2 (LRRK2) are associated with familial Parkinson’s disease (PD). The kinase activity of this complex protein is increased by pathogenic mutations. Inhibition of LRRK2 kinase activity has therefore emerged as
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb913a2423fe06417cb2ecd3e68cdbb8
https://doi.org/10.1016/j.bmcl.2013.02.041
https://doi.org/10.1016/j.bmcl.2013.02.041
Autor:
Chris M. Semko, Danielle L. Aubele, Guriqbal S. Basi, Wes Zmolek, Gary Probst, Matthew N. Mattson, Elizabeth F. Brigham, Erich Goldbach, Karina Wong, William A Wallace, John-Michael Sauer, Hing L. Sham, Lan K. Nguyen, Michael P. Bova, Andrei W. Konradi, Albert W. Garofalo, Susanna S. Hemphill, Darren B. Dressen, Kevin P. Quinn, Minghua Sun, Anh P. Truong, Simeon Bowers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5791-5794
The structure–activity relationship (SAR) of a novel, potent and metabolically stable series of sulfonamide-pyrazoles that attenuate β-amyloid peptide synthesis via γ-secretase inhibition is detailed herein. Sulfonamide-pyrazoles that are efficac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c797a2f9e3d425d83f37dc2fbd3a6ac
https://doi.org/10.1016/j.bmcl.2011.08.008
https://doi.org/10.1016/j.bmcl.2011.08.008
Autor:
John-Michael Sauer, Michael P. Bova, Michael A. Pleiss, Danielle L. Aubele, Elizabeth F. Brigham, Kevin P. Quinn, Balazs G. Szoke, Jennifer Marugg, Wes Zmolek, Andrei W. Konradi, Erich Goldbach, William A Wallace, Guriqbal S. Basi, Martin L. Neitzel, Jacek Jagodzinski, Susanna S. Hemphill
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3715-3720
Herein we describe the structure-activity relationship (SAR) of amino-caprolactam analogs derived from amino-caprolactam benzene sulfonamide 1, highlighting affects on the potency of γ-secretase inhibition, selectivity for the inhibition of APP vers
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::27cb6eff90f380877a438f6c83cf02d4
https://doi.org/10.1016/j.bmcl.2011.04.079
https://doi.org/10.1016/j.bmcl.2011.04.079
Autor:
Xiaocong M, Ye, Andrei W, Konradi, Jenifer, Smith, Danielle L, Aubele, Albert W, Garofalo, Jennifer, Marugg, Marty L, Neitzel, Chris M, Semko, Hing L, Sham, Minghua, Sun, Anh P, Truong, Jing, Wu, Hongbin, Zhang, Erich, Goldbach, John-Michael, Sauer, Elizabeth F, Brigham, Michael, Bova, Guriqbal S, Basi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3502-3506
Significant improvement in metabolic stability on the pyrazolopiperidine scaffold over the original series were achieved and this stability improvement translated in an improved in vivo efficacy.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::864d25ea6d9242d49f72de8a339b07d1
https://doi.org/10.1016/j.bmcl.2010.04.148
https://doi.org/10.1016/j.bmcl.2010.04.148
Autor:
Darren B. Dressen, Ying-Zi Xu, Jenifer L. Smith, Xiaocong M. Ye, Elizabeth F. Brigham, Erich Goldbach, Anh P. Truong, Hing L. Sham, Michael P. Bova, Jennifer Marugg, Guriqbal S. Basi, Jacek Jagodzinski, Hongbin Zhang, Michael A. Pleiss, Andrei W. Konradi, Albert W. Garofalo, John-Michael Sauer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2195-2199
Discovery of a series of pyrazolopiperidine sulfonamide based gamma-secretase inhibitors and its SAR evolution is described. Significant increases in APP potency on the pyrazolopiperidine scaffold over the original N-bicyclic sulfonamide scaffold wer
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0387338b2339269ae539bce793e3d886
https://doi.org/10.1016/j.bmcl.2010.02.039
https://doi.org/10.1016/j.bmcl.2010.02.039
Autor:
Elizabeth F. Brigham, Karen S. Chen, Stephen B. Freedman, Ruth Motter, Weiqun Liu, Manuel Buttini, John P. Anderson, Lisa McConlogue, Sukanto Sinha, Kelly Johnson-Wood, Dora Games, Michael K. Lee, Michelle Zeller
Publikováno v:
Journal of Biological Chemistry. 282:26326-26334
The aspartyl protease beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) initiates processing of amyloid precursor protein (APP) into amyloid beta (Abeta) peptide, the major component of Alzheimer disease (AD) plaques. To determine the rol
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c3db05cead87c83caac2caa1064e167
https://doi.org/10.1074/jbc.m611687200
https://doi.org/10.1074/jbc.m611687200
Autor:
Steven Estus, Elizabeth F. Brigham, Sarah Wright, Russell E. Rydel, H. Michael Tucker, Corlia van Rooyen, Mark Wogulis
Publikováno v:
The Journal of Neuroscience. 17:7736-7745
To gain a molecular understanding of neuronal responses to amyloid-β peptide (Aβ), we have analyzed the effects of Aβ treatment on neuronal gene expressionin vitroby quantitative reverse transcription-PCR andin situhybridization. Treatment of cult
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b254eed90b8681b4dd6810fc77441e3a
https://doi.org/10.1523/jneurosci.17-20-07736.1997
https://doi.org/10.1523/jneurosci.17-20-07736.1997