Zobrazeno 1 - 10
of 42
pro vyhledávání: '"Stefanus J. Steyn"'
Autor:
Zhen Chen, Jiahui Chen, Laigao Chen, Chi-Hyeon Yoo, Jian Rong, Hualong Fu, Tuo Shao, Karen Coffman, Stefanus J. Steyn, April T. Davenport, James B. Daunais, Ahmed Haider, Lee Collier, Lee Josephson, Hsiao-Ying Wey, Lei Zhang, Steven H. Liang
Publikováno v:
Journal of Medicinal Chemistry. 66:1712-1724
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6d6c64f6296ede2568d7df7103162b79
https://doi.org/10.1021/acs.jmedchem.2c00551
https://doi.org/10.1021/acs.jmedchem.2c00551
Autor:
Manthena V.S. Varma, Stefanus J. Steyn
Publikováno v:
Molecular Pharmaceutics. 17:3024-3032
Cytochrome-P450 (P450) isoforms are major drug-metabolizing enzymes implicated in the clearance and drug-drug interactions (DDIs) of diverse small-molecule drugs. Here, we evaluated the association between primary physicochemical descriptors of subst
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::016ca09397d4df1ce60bdc0a2ad8ffad
https://doi.org/10.1021/acs.molpharmaceut.0c00444
https://doi.org/10.1021/acs.molpharmaceut.0c00444
Autor:
Christopher R Butter, Joshua Moon, John F. Harms, Stefanus J. Steyn, John T. Lazzaro, Rebecca E. O’Connor, Catherine A. Thorn, Clinton A Bourbonais, Eda Stark, Jeremy R. Edgerton, Michael Popiolek
Publikováno v:
ACS Chemical Neuroscience. 10:1753-1764
Preclinical and clinical data suggest that muscarinic acetylcholine receptor activation may be therapeutically beneficial for the treatment of schizophrenia and Alzheimer's diseases. This is best exemplified by clinical observations with xanomeline,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9025a7351ef105457c2ee5a26339b5c2
https://doi.org/10.1021/acschemneuro.8b00625
https://doi.org/10.1021/acschemneuro.8b00625
Publikováno v:
ACS Chemical Neuroscience. 9:2832-2837
Cognitive decline and psychosis have been hypothesized to be mediated by N-methyl-d-aspartate receptor (NMDAR) hypofunction. Consistent with this hypothesis, chronic treatment with d-alanine, a coagonist at the glycine site of the NMDAR, leads to an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::791c98a2c48b45ca086045d9bd5aa4d4
https://doi.org/10.1021/acschemneuro.8b00229
https://doi.org/10.1021/acschemneuro.8b00229
Autor:
Anthony R. Harris, Susan M. Lotarski, Michael Aaron Brodney, Michael Popiolek, Catherine A. Thorn, Stephen Jenkinson, Che Wah Lee, Jennifer E. Davoren, Stefanus J. Steyn, Lei Zhang, Terrence Peter Kenakin, Betty Pettersen, Sarah Grimwood, Damien Webb, Michelle R. Garnsey, Simeon Ramsey, John T. Lazzaro, Steven Victor O'neil, Lisa Nottebaum, Jean-Philippe Fortin, Jeremy R. Edgerton
Publikováno v:
Journal of Medicinal Chemistry. 60:6649-6663
Recent data demonstrated that activation of the muscarinic M1 receptor by a subtype-selective positive allosteric modulator (PAM) contributes to the gastrointestinal (GI) and cardiovascular (CV) cholinergic adverse events (AEs) previously attributed
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e16d6e6b4f8608876f69c7501545a8c8
https://doi.org/10.1021/acs.jmedchem.7b00597
https://doi.org/10.1021/acs.jmedchem.7b00597
Autor:
Susan M. Lotarski, Sarah Grimwood, Michael Popiolek, Veronica Reinhart, Jeremy R. Edgerton, Jennifer E. Davoren, Stefanus J. Steyn, John F. Harms, David P. Nguyen
Publikováno v:
Biochemistry. 55:7073-7085
The rationale for using M1 selective muscarinic acetylcholine receptor activators for the treatment of cognitive impairment associated with psychiatric and neurodegenerative disease is well-established in the literature. Here, we investigate measurem
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e7d948042e32f463780f579df4556d74
https://doi.org/10.1021/acs.biochem.6b00688
https://doi.org/10.1021/acs.biochem.6b00688
Autor:
Anthony A. Estrada, Brian K. Fiske, Karin Rudolph, Paul Galatsis, Stephen A. Ploch, Ellis M, Yu H, Zhizhang Yin, Dianne K. Bryce, Matthew L. Maddess, Antonia F. Stepan, Stefanus J. Steyn, Alok K. Sharma, Christopher Houle, Trost C, Carrie G. Markgraf, Warren D. Hirst, Xiang Wang, Ted Barrett, Marco A. S. Baptista, Todd Sherer, Susan E. Hill, Kalpana M. Merchant, William A. Meier, Matthew E. Kennedy, Hong Mei, Xingrong Liu, Christopher Royer, Reina N. Fuji, Matthew J. Fell, Anastasia G. Henry
Putative gain-of-function mutations in leucine-rich repeat kinase 2 (LRRK2), resulting in increased kinase activity and cellular toxicity, are a leading genetic cause of Parkinson’s disease (PD). Hence, there is strong interest in developing LRRK2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4465f413546427102589d503f22b2061
Autor:
João Paulo Lima Daher, Andrew B. West, Warren D. Hirst, Stefanus J. Steyn, Mark S. Moehle, Hisham Abdelmotilib, Laura A. Volpicelli-Daley, Elie Needle, Xianzhen Hu, Paul Galatsis, Yi Chen, Kyle B. Fraser
Publikováno v:
Journal of Biological Chemistry. 290:19433-19444
Therapeutic approaches to slow or block the progression of Parkinson disease (PD) do not exist. Genetic and biochemical studies implicate α-synuclein and leucine-rich repeat kinase 2 (LRRK2) in late-onset PD. LRRK2 kinase activity has been linked to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::33003aa29a17b64485ee9ab6c36fa2bd
https://doi.org/10.1074/jbc.m115.660001
https://doi.org/10.1074/jbc.m115.660001
Publikováno v:
Pharmaceutical Research. 32:3785-3802
Early prediction of clearance mechanisms allows for the rapid progression of drug discovery and development programs, and facilitates risk assessment of the pharmacokinetic variability associated with drug interactions and pharmacogenomics. Here we p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b59ecc6f1503ab70817ffd9552088414
https://doi.org/10.1007/s11095-015-1749-4
https://doi.org/10.1007/s11095-015-1749-4
Autor:
Chakrapani Subramanyam, Gregory W. Kauffman, Patrick B. Mullins, Longfei Xie, Stefanus J. Steyn, John M. Humphrey, Eddie Yang, Patrick Robert Verhoest, Beth C. Vetelino, Tuan P. Tran, Butler Todd W, Benjamin Adam Fish, Martin Pettersson, Kelly R. Bales, Antonia F. Stepan, Christopher J. O’Donnell, Cory Michael Stiff, Kathleen M. Wood, Michael Eric Green, Douglas S. Johnson, Leslie R. Pustilnik, Christopher W. am Ende
Publikováno v:
ACS Medicinal Chemistry Letters. 6:596-601
Herein we describe the design and synthesis of a series of pyridopyrazine-1,6-dione γ-secretase modulators (GSMs) for Alzheimer's disease (AD) that achieve good alignment of potency, metabolic stability, and low MDR efflux ratios, while also maintai
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf675492957abbcaed313fb175f827aa
https://doi.org/10.1021/acsmedchemlett.5b00070
https://doi.org/10.1021/acsmedchemlett.5b00070