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Vincent Peterkin

Explore the profile of Vincent Peterkin including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 7
Citations 416
Followers 0
Related Specialties
Biochemistry
Pharmacology
Chemistry
Top 10 Co-Authors
Preethi Krishnan
Hui-Ju Chen
J Andrew Williams
Daniel A J Bow
Rolf Wagner
A Chris Krueger
Tatyana Dekhtyar
Theunis C Goosen
Tongmei Li
John T Randolph
Published In
Drug Metab Dispos
Bioorg Med Chem
Biochem J
Bioorg Med Chem Lett
Comb Chem High Throughput Screen
Affiliations
Soon will be listed here.
Recent Articles
1.
Discovery of 2-aminoisobutyric acid ethyl ester (AIBEE) phosphoramidate prodrugs for delivering nucleoside HCV NS5B polymerase inhibitors
Randolph J, Li T, Krueger A, Heyman H, Chen H, Bow D, et al.
Bioorg Med Chem Lett . 2020 Feb; 30(7):126986. PMID: 32046903
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 profile...
2.
Synthesis and evaluation of 2'-dihalo ribonucleotide prodrugs with activity against hepatitis C virus
Krueger A, Chen H, Randolph J, Brown B, Halvorsen G, Heyman H, et al.
Bioorg Med Chem . 2019 Nov; 28(1):115208. PMID: 31740203
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 activity...
3.
A High Throughput, 384-Well, Semi-Automated, Hepatocyte Intrinsic Clearance Assay for Screening New Molecular Entities in Drug Discovery
Heinle L, Peterkin V, de Morais S, Jenkins G, Badagnani I
Comb Chem High Throughput Screen . 2015 Apr; 18(5):442-52. PMID: 25828461
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...
4.
Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1
Schnute M, McReynolds M, Kasten T, Yates M, Jerome G, Rains J, et al.
Biochem J . 2012 Mar; 444(1):79-88. PMID: 22397330
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...
5.
A humanized UGT1 mouse model expressing the UGT1A1*28 allele for assessing drug clearance by UGT1A1-dependent glucuronidation
Cai H, Nguyen N, Peterkin V, Yang Y, Hotz K, La Placa D, et al.
Drug Metab Dispos . 2010 Feb; 38(5):879-86. PMID: 20124398
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...
6.
Udp-glucuronosyltransferase 2b7 is the major enzyme responsible for gemcabene glucuronidation in human liver microsomes
Bauman J, Goosen T, Tugnait M, Peterkin V, Hurst S, Menning L, et al.
Drug Metab Dispos . 2005 Jun; 33(9):1349-54. PMID: 15980101
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...
7.
Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios
Williams J, Hyland R, Jones B, Smith D, Hurst S, Goosen T, et al.
Drug Metab Dispos . 2004 Aug; 32(11):1201-8. PMID: 15304429
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...