Search results for: Michael B. Fisher

Items from 1 to 14 out of 14 results

article

Rapid Detection of Escherichia coli in Water Using Sample Concentration and Optimized Enzymatic Hydrolysis of Chromogenic Substrates

Jianyong Wu, Jill R. Stewart, Mark D. Sobsey, Chris Cormency, more

Current Microbiology > 2018 > 75 > 7 > 827-834

Methods for rapid detection of fecal indicator bacteria in water are important to ensure that water is safe for drinking, bathing, recreation, fishing and shellfish harvesting. In this study, we tested experimental conditions for bacterial hydrolysis of two promising enzymatic substrates, 5-Bromo-4-chloro-3-indolyl β-d-glucuronide (X-Gluc) and Resorufin β-d-glucuronide (REG), and optimized parameters...

article

Piperazinyl-oxadiazoles as selective sphingosine-1-phosphate receptor agonists

Joshua C. Horan, Sulagna Sanyal, Younggi Choi, Melissa Hill-Drzewi, more

Bioorganic & Medicinal Chemistry Letters > 2014 > 24 > 20 > 4807-4811

The discovery of a new series of selective S1P ₁ agonists is described. This series of piperazinyl-oxadiazole derivatives was rapidly optimized starting from high-throughput screening hit 1 to afford potent and selective lead compound 10d. Further SAR studies showed that 10d was converted to the active phosphate metabolite 29 in vivo. Oral administration of compound 10d to rats was shown to...

article

Solar water disinfection (SODIS) of Escherichia coli, Enterococcus spp., and MS2 coliphage: Effects of additives and alternative container materials

Michael B. Fisher, Mercedes Iriarte, Kara L. Nelson

Water Research > 2012 > 46 > 6 > 1745-1754

The use of alternative container materials and added oxidants accelerated the inactivation of MS2 coliphage and Escherichia coli and Enterococcus spp. bacteria during solar water disinfection (SODIS) trials. Specifically, bottles made from polypropylene copolymer (PPCO), a partially UVB-transparent plastic, resulted in three-log inactivation of these organisms in approximately half the time required...

article

Simulated Sunlight Action Spectra for Inactivation of MS2 and PRD1 Bacteriophages in Clear Water

Michael B. Fisher, David C. Love, Rudi Schuech, Kara L. Nelson

Environmental Science & Technology > 2011 > 45 > 21 > 9249 - 9255

article

Discovery of CP-690,550: A Potent and Selective Janus Kinase (JAK) Inhibitor for the Treatment of Autoimmune Diseases and Organ Transplant Rejection

Mark E. Flanagan, Todd A. Blumenkopf, William H. Brissette, Matthew F. Brown, more

Journal of Medicinal Chemistry > 2010 > 53 > 24 > 8468 - 8484

chapter

Complexities of Working with UDP‐ Glucuronosyltransferases (UGTs): Focus on Enzyme Inhibition

Michael B. Fisher

Enzyme Inhibition in Drug Discovery and Development > Inhibition of the Drug Metabolizing Enzymes—The Undesirable Inhibition > 407 - 422

This chapter contains sections titled: Introduction Introduction to UGT Inhibition Inhibition of UGT Clinical Drug–Drug Interactions AZT as an example to Understand UGT Inhibition in Vitro and in Vivo Putting IT all together: Correct Prediction of Fluconazole–Zidovudine and Valproic Acid–Lamotrigine Interactions Conclusions References

article

Piperazinyl CCR1 antagonists—optimization of human liver microsome stability

Matthew F. Brown, Kevin B. Bahnck, Laura C. Blumberg, William H. Brissette, more

Bioorganic & Medicinal Chemistry Letters > 2007 > 17 > 11 > 3109-3112

The synthesis, biological activity, and pharmacokinetic profile of CCR1 antagonists are described.

article

A streamlined method to predict hepatic clearance using human liver microsomes in the presence of human plasma

Sara M. Skaggs, Robert S. Foti, Michael B. Fisher

Journal of Pharmacological and Toxicological Methods > 2006 > 53 > 3 > 284-290

Human liver microsomal incubations are often used to predict the metabolic lability of new chemical entities. The clearance values are scaled-up from in vitro data and mathematically corrected for plasma protein binding, or in some cases the free fraction ratio of plasma to microsomes, using well-established scaling methods such as the well-stirred model. This can be time consuming for multiple compounds...

article

Assessment of UDP-glucuronosyltransferase catalyzed formation of ethyl glucuronide in human liver microsomes and recombinant UGTs

Robert S. Foti, Michael B. Fisher

Forensic Science International > 2005 > 153 > 2-3 > 109-116

While ethanol is primarily metabolized to acetaldehyde and acetic acid via alcohol dehydrogenase, a minor but increasingly important pathway in the field of forensic science involves the conjugation of glucuronic acid to form an ethyl glucuronide (EtG) metabolite. The kinetics of ethyl glucuronide formation were examined in human liver microsomes (HLM) and recombinant UDP-glucuronosyltransferases...

article

Active Site Characteristics of CYP4B1 Probed with Aromatic Ligands ^†

Kirk R. Henne, Michael B. Fisher, Krishna R. Iyer, Dieter H. Lang, more

Biochemistry > 2001 > 40 > 29 > 8597 - 8605

article

Immunochemical Identification of UGT Isoforms in Human Small Bowel and in Caco-2 Cell Monolayers

Mary F. Paine, Michael B. Fisher

Biochemical and Biophysical Research Communications > 2000 > 273 > 3 > 1053-1057

Previous work had suggested the presence of significant levels of UDP-glucuronosyltransferase 1A1 (UGT1A1) catalytic activity in human small intestinal microsomes, with undetectable to low UGT1A6 and 2B7 activities. To confirm the presence of UGT1A1 isoform in human small bowel, to explore the possible absence of UGT1A6 and 2B7 in the organ, and to examine induced Caco-2 cells as a potential model...

article

P450-Catalyzed In-Chain Desaturation of Valproic Acid: Isoform Selectivity and Mechanism of Formation of Δ ³ -Valproic Acid Generated by Baculovirus- Expressed CYP3A1

Michael B. Fisher, Stella J. Thompson, Vera Ribeiro, Maria C. Lechner, more

Archives of Biochemistry and Biophysics > 1998 > 356 > 1 > 63-70

The mechanism of formation of the in-chain, unsaturated fatty acid metabolite, Δ ³ -valproic acid (Δ ³ -VPA) by rat liver microsomes was examined. Microsomal rates of formation of Δ ³ -VPA were below quantifiable limits in reactions catalyzed by control female rat liver microsomes, but were induced more than 20-fold following pretreatment with triacetyloleandomycin and pregnenolone-16α-carbonitrile...

article

Positional Specificity of Rabbit CYP4B1 for ω-Hydroxylation1of Short-Medium Chain Fatty Acids and Hydrocarbons

Michael B. Fisher, Yi-Min Zheng, Allan E. Rettie

Biochemical and Biophysical Research Communications > 1998 > 248 > 2 > 352-355

Rabbit CYP4B1 was incubated with a series of fatty acid and hydrocarbon substrates and metabolites were identified by gas chromatography and gas chromatography/mass spectrometry. C-7 to C-10 n-alkyl fatty acids were preferentially hydroxylated at the terminal carbon (ω/ω-1 = 1.1–7.4) with turnover numbers of 1–11 min⁻¹. The C-7 to C-10 n-alkyl hydrocarbons exhibited turnover numbers of 11–33 min⁻¹...

article

Prochiral sulfide probes for the active-site topography of rabbit flavin-containing monooxygenase 2 (FMO2)

Michael B. Fisher, Allan E. Rettie

Tetrahedron: Asymmetry > 1997 > 8 > 4 > 613-618

Mammalian flavin-containing monooxygenases are known to oxygenate prochiral sulfides often with a high degree of stereoselectivity. In the present study we used two homologous series of n-alkyl aryl sulfides, Ar-S-(CH ₂ ) _n H, (where Ar=p-tolyl or 2-naphthyl and n=1-7), to probe the active site topography of rabbit lung FMO2. Purified FMO2 was incubated with each member of the the...

Filter options

Publication date

Set your own date range

INFONA - science communication portal

Search results for: Michael B. Fisher

Add recipient

Sending message cancelled

Are you sure you want to cancel sending this message?

Send message

Filter options

Publication date

Date range setting

Set the date range to filter the displayed results. You can set a starting date, ending date or both. You can enter the dates manually or choose them from the calendar.

Content availability

Publication type

Keywords

Data set

Journal

Reporting an error / abuse

Sending the report failed

Accessibility options