Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Vincent Peterkin"'
Autor:
Preethi Krishnan, Rodger F. Henry, Christopher C. Marvin, Tatyana Dekhtyar, Rolf Wagner, John T. Randolph, A. Chris Krueger, David A. Degoey, Vincent Peterkin, Michelle Irvin, Geoff T. Halvorsen, Jason P. Shanley, Heyman Howard R, Eric A. Voight, Robert A. Carr, Cecilia Van Handel, Tongmei Li, Brian S. Brown, Daniel A.J. Bow, Hui-Ju Chen, DeAnne Stolarik
Publikováno v:
Bioorganicmedicinal chemistry. 28(1)
Download : Download high-res image (149KB) Download : Download full-size image Hepatitis C virus (HCV) nucleoside inhibitors have been a key focus of nearly 2 decades of HCV drug research due to a high barrier to drug resistance and pan-genotypic act
Autor:
John T. Randolph, Vincent Peterkin, Robert A. Carr, David A. Degoey, Tongmei Li, Daniel A.J. Bow, Hui-Ju Chen, Preethi Krishnan, DeAnne Stolarik, Rolf Wagner, Cecilia Van Handel, Michelle Irvin, A. Chris Krueger, Heyman Howard R, Tatyana Dekhtyar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:126986
Our HCV research program investigated novel 2′-dihalogenated nucleoside HCV polymerase inhibitors and identified compound 1, a 5′-phosphoramidate prodrug of 2′-deoxy-2′-α-bromo-β-chloro uridine. Although 1 had a favorable in vitro activity
Publikováno v:
Combinatorial Chemistry & High Throughput Screening. 18:442-452
A high throughput, semi-automated clearance screening assay in hepatocytes was developed allowing a scientist to generate data for 96 compounds in one week. The 384-well format assay utilizes a Thermo Multidrop Combi and an optimized LC-MS/MS method.
1. Accurate predictions of clinical transporter-mediated drug–drug interactions (DDI) from in vitro data can be challenging when compounds have poor solubility and/or high nonspecific binding. Additionally, current DDI predictions for compounds wit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bba88741010ee581108278652122b17b
Autor:
Michelle Kraus, Jay M. Wendling, Olga V. Nemirovskiy, John W. Rains, Vincent Peterkin, Laura E. Zawadzke, Hideji Fujiwara, Ciarán N. Cronin, Troii Hall, Tom Kasten, Maureen K. Highkin, Gina M. Jerome, Arthur J. Wittwer, Matthew P. Yates, Shinji Ogawa, Jeffrey A. Scholten, Jill Chrencik, Marek M. Nagiec, Matthew D. McReynolds, Kaliapan Iyanar, Mark E. Schnute, Kristin Cukyne, Matthew J. Saabye, Richard M. Broadus
Publikováno v:
Biochemical Journal. 444:79-88
SphK (sphingosine kinase) is the major source of the bioactive lipid and GPCR (G-protein-coupled receptor) agonist S1P (sphingosine 1-phosphate). S1P promotes cell growth, survival and migration, and is a key regulator of lymphocyte trafficking. Inhi
Autor:
Hongliang Cai, Nghia Nguyen, Deirdre Beaton La Placa, Shujuan Chen, Vincent Peterkin, Robert H. Tukey, Kathy Hotz, Young Sun Yang, Jeffrey C. Stevens
Publikováno v:
Drug Metabolism and Disposition. 38:879-886
Humanized mice that express the human UDP-glucuronosyltransferase (UGT) 1 locus have been developed in a Ugt1-null background as a model to improve predictions of human UGT1A-dependent drug clearance. Enzyme kinetic parameters (K(m) and V(max)) and p
Autor:
Jonathan N. Bauman, Theunis C. Goosen, Michael Z. Man, Scott P. Myrand, Joseph Paulauskis, Vincent Peterkin, J. Andrew Williams, Lee C. Menning
Publikováno v:
British Journal of Clinical Pharmacology. 64:458-468
What is already known about this subject • The UGT1A1*28 polymorphism is known to reduce UGT1A1 enzyme activities, via an extra TA repeat in the promoter. • However, a gap exists with regard to a comprehensive assessment of the influence of this
Autor:
Theunis C. Goosen, Susan Hurst, Mark Milad, J. Andrew Williams, Meera Tugnait, Michael H. Court, Lee C. Menning, Vincent Peterkin, Jonathan N. Bauman
Publikováno v:
Drug Metabolism and Disposition. 33:1349-1354
The predominant metabolic pathway of gemcabene in humans is glucuronidation. The principal human UDP-glucuronosyltransferases (UGTs) involved in the glucuronidation of gemcabene were determined in this study. Glucuronidation of gemcabene was catalyze
Autor:
Dennis A. Smith, Susan Hurst, J. Andrew Williams, Theunis C. Goosen, Simon E. Ball, Barry Jones, Vincent Peterkin, Jeffrey R. Koup, Ruth Hyland
Publikováno v:
Drug Metabolism and Disposition. 32:1201-1208
Glucuronidation is a listed clearance mechanism for 1 in 10 of the top 200 prescribed drugs. The objective of this article is to encourage those studying ligand interactions with UDP-glucuronosyltransferases (UGTs) to adequately consider the potentia