Latest Posters
Poster
Metabolic Stability and Clearance of Pharmaceutical Chemicals in Pre-Pooled Cryopreserved Hepatocytes
Cryopreserved hepatocytes express both phase I and phase II enzymes and facilitate early evaluation of the metabolic stability of pharmaceuticals. Availability of pre-pooled cryopreserved hepatocytes further enhances the utility of this model by reducing donor to donor variability. In this study, the metabolic stability of 29 pharmaceutical compounds were evaluated in pre-pooled cryopreserved human hepatocytes.
Poster
Extract Optimum Value from Screening data using a Modern Complete Screening Solution
With the use of numerous standardized biochemical assays now commonplace, successful application of screening technologies requires accurate and meaningful handling of the experimental results. Specifically, this means capturing the vast data volumes generated and subsequent validation and verification. Decision making can be supported via comprehensive and intuitive visualization of results.
Poster
CyTRAK™ Probes: Novel Nuclear and Cytoplasm Discriminators Compatible with GFP-Based HCS and HTS Assays
Image-based high-content screening assays, demand solutions for image segmentation and cellular compartment encoding to track critical events – for example those presented by GFPreporters within cell cycle tracking and GPCR translocation assays. We have designed nuclear and cytoplasm discriminator CyTRAK™ probes - spectrally compatible with all variants of GFPreporters offering new solutions in cytometry.
Poster
A novel Hydrogel Mountant - CyGEL™ - Enables Temporospatial HCS Imaging Assays of Live non-Adherent Cells
New technologies are needed to deal with live cell-based HCS assays on non-adherent cells or to exploit suspension cells in fluidic systems. Here we describe CyGEL™ - a thermo-reversible hydrogelbased 4-D immobilization technology for live cell location without imposing an anchoring to a substrate.
Poster
An Ultra-Sensitive Fluorimetric Assay for the Detection of Renin Activity
To facilitate high throughput screening of renin inhibitors, we have developed new renin assay kits utilizing FRET peptide substrates. The SensoLyte™ 520 Renin Assay Kit contains FRET peptide labeled with the quencher QXL™520 and the fluorophore 5-FAM. These newly developed assays were validated with several known renin inhibitors. Assay with QXL™ 520/5-FAM substrate was approximately 40 fold more sensitive than an existing assay which uses EDANS/DABCYL FRET substrate.
Poster
Design and Synthesis of Novel Thiazolidine and Pyrrolidine Derivatives as DPP-IV Inhibitors
DPP-IV inhibitors have many advantages like increasing insulin release and suppressing glucagon release in a glucose-dependent manner hence they pose less of a hypoglycemia risk and no weight gain than that observed with other antihyperglycemic agents. To develop a novel potent DPP-IV inhibitors we have synthesized and evaluated DPP-IV inhibiting activity and selectivity of various compounds. All these results would facilitate further development of Novel drugs for treatment of type 2 diabetes.
Poster
CYP4F Enzymes are the Major Enzymes in Human Liver Microsomes that Catalyze the O-Demethylation of the Antiparasitic Prodrug DB289
DB289 is a prodrug that is converted by several steps to the active metabolite DB75. DB289 exhibits enhanced oral efficacy and reduced acute toxicity over DB75, an aromatic dicationic compound that is effective against a broad range of pathogens in vitro including African trypanosomiasis (African sleeping sickness). This reaction phenotyping study aimed to identify the enzymes responsible for oxidative O-demethylation; the first step in this conversion to DB75.
Poster
Alfentanil N-deakylation: Monitoring the Formation of N-phenylpropionamide (AMX) to Determine CYP3A4 Activity in Vitro
Alfentanil is a synthetic analgesic cleared exclusively by hepatic metabolism. Due to the highly linear correlation between alfentanil systemic clearance and CYP3A4 activity, as well as the direct pharmacologic effects on pupil size, it has been used as a non-invasive metabolic probe for CYP3A4 activity in vivo. AMX is a direct metabolite of alfentanil, evaluated in this study for its potential to measure CYP3A4 activity in vitro.
Poster
Effects of Gender, age and Ethnicity on Human Cytochrome P450 Activity
The expression of CYP enzymes is influenced by both endogenous and exogenous factors. The aim of this analysis was to evaluate whether the age, gender, or ethnicity of the donor should influence the selection of human liver microsomes for drug metabolism studies, as well as whether cigarette smoking and alcohol consumption are reliable indicators of elevated CYP1A2 and CYP2E1 activity, respectively.
Poster
Kinetic Constants and Sample-to-Sample Variation in the Rate of Metabolism of two or more Substrates for Human Liver Microsomal CYP1A2, CYP2B6, CYP2C8, CYP2D6 and CYP3A4/5
Marker substrates for certain CYPs have changed for several reasons, including the need for improved selectivity and sensitivity, reliable substrates for LC/MS/MS analysis, and substrates that provide greater repeatability. The objectives of this study were to compare sample-to-sample variation in cytochrome P450 enzymatic rates between two or more CYP-specific substrates and to determine Michaelis-Menten kinetic constants for these same reactions using a pool of human liver microsomes.
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