Fluorescent High Throughput P450 Assays
High Throughput P450 Inhibition Kits
These human Cytochrome P450 High Throughput Inhibitor Screening Kits
are designed to rapidly screen for potential inhibitors of human P450 catalytic
activity. Each kit provides all the necessary components and instructions
for measuring the IC50 value of up to 38 test compounds in 96-well plates.
The inhibitor screening kit includes the following components: recombinant
human P450 (BD Supersomes™), fluorescent P450 substrate, positive control
inhibitor, metabolite standard, NADPH regenerating system, reaction buffer,
stop reagent, control membrane protein, and an instruction manual. Learn
more >>
Follow these links to learn more about high throughput screening
methodology for human cytochrome P450 inhibition.
Posters
Papers
- Stresser DM (2004) High-throughput screening of human cytochrome P450
inhibitors using fluorometric substrates: Methodology for 25 enzyme
substrate pairs. In “Optimization in Drug Discovery: In Vitro Methods”
(Z. Yan and G. W. Caldwell eds) in series “Methods in Pharmacology
and Toxicology (YJ Kang, series ed), Humana press, Totowa, NJ, USA
- Ekins S, Stresser DM and Williams JA (2003) In vitro and pharmacophore
insights for CYP3A enzymes. Trends Pharm. Sci. 24: 161-166
- Kragie L, Turner SD, Patten CJ, Crespi CL and Stresser DM (2002) Assessing
pregnancy risks of azole antifungals using a high throughput aromatase
inhibition assay. Endocrine Research, 28: 129-140.
- Crespi CL, Miller VP and Stresser DM (2002) Design and application
of fluorometric assays for human cytochrome P450 inhibition. Methods
in Enzymology 357:276-284.
- Yamamoto, T, Suzuki, A and Kohno, Y. (2002) Application of Microtiter
Palte Assay to Evaluate Inhibitory Effects of Various Compounds on Nine
Cytochrome P450 Isoforms and to Estimate their Inhibition Patterns.
Drug metabol. Pharmacokin. 17(5):437-448.
- Chauret N, Dobbs B, Lackman RL, Bateman K, Nicoll-Griffith DA, Stresser
DM, Ackermann JA, Turner SD, Miller VP and Crespi CL (2001) The use
of 3-[2-(N,N-diethyl-N-methylammonium)ethyl]-7-methoxy-4-methylcoumarin
(AMMC) as a specific CYP2D6 probe in human liver microsomes. Drug
Metab Dispos. 29:1196-1200.
- Crespi CL, and Stresser DM (2000) Fluorometric screening for metabolism-based
drug-drug interactions. J Pharmacol Toxicol Methods, 44(1):325-31.
- Stresser DM, Blanchard AP, Turner SD, Erve JCL, Dandeneau AA, Miller
VP and Crespi CL (2000) Substrate-dependent modulation of CYP3A4 catalytic
activity: analysis of 27 test compounds with four fluorometric substrates.
Drug Metab Dispos. 28: 1440-1448.
- Design, Synthesis, and Characterization of 7-Methoxy-4-(aminomethyl)coumarin
as a Novel and Selective Cytochrome P450 2D6 Substrate Suitable for
High-Throughput Screening Onderwater RCA, Venhorst J, Commandeur JNM
and Vermeulen NPE Chem.
Res. Toxicol. (1999) 12:555-559.
- Higher-throughput Screening With Human Cytochromes P450 Crespi CL
Current Opinion in Drug Discovery & Development (1999) 2(1):15-19.
- Effects of Ginseng Components on cDNA-Expressed Cytochrome P450 Enzyme
Catalytic Activity
Henderson GL, Harkey MR, Gershwin ME, Hackman RM, Stern JS and Stresser
DM, Life Sci. (1999) 65(15):209-214.
- High Throughput Screening for Inhibition of Cytochrome P450 Metabolism
Crespi CL, Miller VP and Penman BW, Med. Chem. Res. (1998) 8(7/8): 457-471.
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