Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Nancy A Sachs"'
Autor:
Zhijian Zhao, Nathan R. Kett, Sujata Sharma, James C. Barrow, Robert F. Smith, Jeffrey W. Schubert, Nancy A. Sachs, Scott E. Wolkenberg, Ronald G. Robinson, Jeffrey Y. Melamed, Michael S. Poslusney, James Mulhearn, Pete H. Hutson, Scott T. Harrison, Dawn L. Hall, John M. Sanders, Timothy J. Allison, Sangita B. Patel
Publikováno v:
ACS Medicinal Chemistry Letters. 6:318-323
3-Hydroxy-4-pyridinones and 5-hydroxy-4-pyrimidinones were identified as inhibitors of catechol-O-methyltransferase (COMT) in a high-throughput screen. These heterocyclic catechol mimics exhibit potent inhibition of the enzyme and an improved toxicit
Autor:
Jay A. Grobler, Meizhen Feng, Yuan Li, Yves Ducharme, Jean-Pierre Falgueyret, Bernard Cote, Youwei Yan, Louis-Charles Campeau, Ernest Asante-Appiah, Ming-Tain Lai, Jason Burch, Marc V. Witmer, Daria J. Hazuda, Michael D. Miller, Nancy A. Sachs, Elizabeth Cauchon, Paul Tawa, Daniel J. DiStefano, Meiqing Lu
Publikováno v:
Antimicrobial Agents and Chemotherapy. 58:1652-1663
Nonnucleoside reverse transcriptase inhibitors (NNRTIs) are a mainstay of therapy for treating human immunodeficiency type 1 virus (HIV-1)-infected patients. MK-1439 is a novel NNRTI with a 50% inhibitory concentration (IC 50 ) of 12, 9.7, and 9.7 nM
Autor:
Christopher R. Gibson, Stacey L. Polsky-Fisher, Lihang Yao, Nanyan Rena Zhang, Ronald G. Robinson, Jeffrey W. Schubert, John M. Sanders, Scott E. Wolkenberg, Pete H. Hutson, Nancy A. Sachs, Scott T. Harrison, Debra McLoughlin, Zhijian Zhao, James C. Barrow, Sean M. Smith, Monika Kandebo
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(12)
A series of N -heterocyclic pyridinone catechol- O -methyltransferase (COMT) inhibitors were synthesized. Physicochemical properties, including ligand lipophilic efficiency (LLE) and c log P , were used to guide compound design and attempt to improve
Autor:
Ming-Tain Lai, Nancy A. Sachs, Min Xu, Jay A. Grobler, Michael D. Miller, Daria J. Hazuda, Wade Blair, Meizhen Feng
Publikováno v:
Antimicrobial agents and chemotherapy. 60(4)
Doravirine (DOR), which is currently in a phase 3 clinical trial, is a novel human immunodeficiency type 1 virus (HIV-1) nonnucleoside reverse transcriptase inhibitor (NNRTI). DOR exhibits potent antiviral activity against wild-type virus and K103N,
Autor:
Ronald G. Robinson, Kausik K. Nanda, B. Wesley Trotter, Pete H. Hutson, Monika Kandebo, James Mulhearn, Debra McLoughlin, Sean M. Smith, Stacey L. Polsky-Fisher, Tiffany L. Walker, Jennifer L. Kershner, Peter J. Manley, Neetesh Bhandari, Nancy A. Sachs, James C. Barrow, Dawn L. Hall, Zhijian Zhao, Scott T. Harrison, Lihang Yao, Robert F. Smith, John M. Sanders, Christopher R. Gibson, Sujata Sharma, Jeffrey W. Schubert, Scott E. Wolkenberg
Publikováno v:
ACS Chemical Neuroscience. 3:129-140
Reduced dopamine neurotransmission in the prefrontal cortex has been implicated as causal for the negative symptoms and cognitive deficit associated with schizophrenia; thus, a compound which selectively enhances dopamine neurotransmission in the pre
Autor:
R. Bednar, Xiaoping Zhang, Sophie Parmentier-Batteur, Jason M. Uslaner, C. Gambone, G. Xu, Mario Guzzi, Peter H. Hutson, W. Le-Mair, P.E. Sanderson, Robert Mazzola, Nancy A. Sachs, Brian C. Magliaro, Lynn A. Hyde, Deborra Mullins, Michael J. Marino, Antonella Converso, Sean M. Smith, B.K. Eschle, Donnie Eddins, Jeffrey A. Vivian, H. Sloan, Diane Rindgen, E.N. Finger, A. Wang, Zachary A. Turnbull
Publikováno v:
Neuropharmacology. 61:665-676
Inhibition of phosphodiesterase 9 (PDE9) has been reported to enhance rodent cognitive function and may represent a potential novel approach to improving cognitive dysfunction in Alzheimer’s disease. PF-04447943, (6-[(3 S ,4 S )-4-methyl-1-(pyrimid
Autor:
Virginia L. Willour, Devin McQuaid, Heather Bruce, Nancy A. Sachs, Lynn E. DeLisi, Daniel P. Gaile, Jeffrey M. Conroy, Stephanie Lin, Michael R. Rossi, Christopher A. Ross, Norma J. Nowak, Dobrila D. Rudnicki, Pamela Sklar, Susan E. Holmes, John K. Cowell, Russell L. Margolis
Publikováno v:
Psychiatric Genetics. 19:64-71
Objectives Genomic copy number variations (CNVs) are a major form of variation in the human genome and play an etiologic role in several neuropsychiatric diseases. Tandem repeats, particularly with long (>50 bp) repeat units, are a relatively common
Autor:
Nancy A Sachs, Richard R. Vaillancourt
Publikováno v:
Journal of Neurochemistry. 88:51-62
Tyrosine hydroxylase (TH) is regulated by the reversible phosphorylation of serines 8, 19, 31 and 40. Upon initiation of this study, serine 19 was unique due to its requirement of 14-3-3 binding after phosphorylation for optimal enzyme activity, alth
Autor:
Mark A. Nelson, Anne Christine Goulet, Yongmei Feng, Jiaqi Shi, John W.B. Hershey, Richard R. Vaillancourt, Nancy A Sachs
Publikováno v:
Journal of Biological Chemistry. 278:5062-5071
Cyclin-dependent kinase 11 (CDK11; also named PITSLRE) is part of the large family of p34cdc2-related kinases whose functions appear to be linked with cell cycle progression, tumorigenesis, and apoptotic signaling. However, substrates of CDK11 during
Publikováno v:
Archives of Biochemistry and Biophysics. 407:103-116
Much effort has focused on the identification of MAPK cascades that are activated by the MEKK family of protein kinases. However, direct phosphorylation and regulation of the MEKK proteins has not been shown. To address this question, we have express