Zobrazeno 1 - 10
of 56
pro vyhledávání: '"John E. Leet"'
High-throughput screening and rapid inhibitor triage using an infectious chimeric Hepatitis C virus.
Autor:
Michael J Wichroski, Jie Fang, Betsy J Eggers, Ronald E Rose, Charles E Mazzucco, Kevin A Pokornowski, Carl J Baldick, Monique N Anthony, Craig J Dowling, Lauren E Barber, John E Leet, Brett R Beno, Samuel W Gerritz, Michele L Agler, Mark I Cockett, Daniel J Tenney
Publikováno v:
PLoS ONE, Vol 7, Iss 8, p e42609 (2012)
The recent development of a Hepatitis C virus (HCV) infectious virus cell culture model system has facilitated the development of whole-virus screening assays which can be used to interrogate the entire virus life cycle. Here, we describe the develop
Externí odkaz:
https://doaj.org/article/c696c60727114ef3a6359c336e98b64f
Autor:
Xiaohua Stella Huang, Dieter M. Drexler, Xiaoliang Zhuo, John E. Leet, Benjamin M. Johnson, Kyle Parcella, Joseph L. Cantone, Matthew G. Soars, Kathleen W. Mosure, Kap-Sun Yeung, Kyle J. Eastman, Yingzi Wang, John F. Kadow
Publikováno v:
Drug Metabolism and Disposition. 44:1332-1340
During a medicinal chemistry campaign to identify inhibitors of the hepatitis C virus nonstructural protein 5B (RNA-dependent RNA polymerase), a bicyclo[1.1.1]pentane was introduced into the chemical scaffold to improve metabolic stability. The inhib
Publikováno v:
SLAS Discovery. 19:1409-1414
Plastic labware is used in all processes of modern pharmaceutical research, including compound storage and biological assays. The use of these plastics has created vast increases in productivity and cost savings as experiments moved from glass test t
Autor:
Yue-Zhong Shu, Li Ma, Goodrich Jason, R. Marcus Fancher, Makonen Belema, Mingshe Zhu, John E. Leet, W. Griffith Humphreys, Yang Hong, Min Gao, Lopez Omar D, Van N. Nguyen, Benjamin M. Johnson, Weiping Zhao, Wenying Li, Janet Caceres-Cortes, John A. Easter, Shu Y Chang, Xiaohong Liu, Xiaohua Huang, Lawrence G. Hamann
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 44(6)
Daclatasvir is a first-in-class, potent, and selective inhibitor of the hepatitis C virus nonstructural protein 5A replication complex. In support of nonclinical studies during discovery and exploratory development, liquid chromatography-tandem mass
Autor:
Donald R. O'Boyle, Denis R. St. Laurent, Nicholas A. Meanwell, Peter T. Nower, Xiaohua Stella Huang, Jeffrey L. Romine, Michael H. Serrano-Wu, Julie A. Lemm, John E. Leet, Milind Deshpande, Scott W. Martin, Lawrence B. Snyder, Min Gao, Jin-Hua Sun, Fukang Yang
Publikováno v:
ACS Medicinal Chemistry Letters. 2:224-229
The iminothiazolidinone BMS-858 (2) was identified as a specific inhibitor of HCV replication in a genotype 1b replicon assay via a high-throughput screening campaign. A more potent analogue, BMS-824 (18), was used in resistance mapping studies, whic
Autor:
John E. Leet, Ravindra W. Tejwani, Louis J. Lombardo, Yueping Zhang, Benjamin M. Johnson, Xiaohong Liu, Rajeev S. Bhide, Donna D. Wei, Ligang Qian, Yue-Zhong Shu, Amrita Kamath
Publikováno v:
Drug Metabolism and Disposition. 36:2475-2483
5-Isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737) is a potent and selective vascular endothelial growth factor receptor-2 antagonist. In this study, liquid chroma
Autor:
Xiaohong Liu, Raouf Hussain, David J. Newman, John E. Leet, Craig R. Fairchild, Stella Huang, Dieter M. Drexler, Stephen W. Mamber, David G. I. Kingston, Joseph L. Cantone
Publikováno v:
Journal of Natural Products. 71:460-463
Two new cytotoxic xanthones were isolated from extracts of the Madagascar rain forest plant Psorospermum cf. molluscum using bioassay guided fractionation with the Escherichia coli SOS chromotest. The structures of the new dihydrofuranoxanthones, des
Publikováno v:
Magnetic Resonance in Chemistry. 45:447-450
We report here the observation of OH…N hydrogen-bond 1hJN, OH scalar coupling in a biologically active natural product. The intramolecular hydrogen bond between the threonine hydroxyl (Thr-OH) group and the thiazolyl nitrogen at the second thiazole
Autor:
Clotilde Bourin, John F. McElroy, John E. Leet, David A. Stock, John B. Hogan, Frederic Machet, Ping Chen, Mark D. Lindner
Publikováno v:
Experimental and Clinical Psychopharmacology. 14:42-51
Amitriptyline and gabapentin are the primary treatments for painful diabetic neuropathy (PDN), and it is clear that they produce beneficial effects, but there are questions about these treatments that have not been adequately addressed. For example,
Autor:
Michael J. Pucci, Goodrich Jason, Junius M. Clark, Alicia Regueiro-Ren, Timothy P. Connolly, Joanne J. Bronson, Dane M. Springer, Xiaohua Stella Huang, John E. Leet, Yasutsugu Ueda
Publikováno v:
Journal of Natural Products. 68:550-553
Nocathiacin I (1) was converted to its deoxy indole analogue, nocathiacin II (2), another natural product, by a unique and facile chemical process. This process was applied to nocathiacin IV (4), generating the lactone analogue of glycothiohexide alp