Latest Posters
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.
Poster
Pharmacophore Mapping of Flavone Derivatives for Aromatase Inhibiton
The study explores the structural requirements of flavones for inhibition of aromatase activity. The QSAR analysis generates the model that shows the importance of flavone ring and with molecular lipophilicity. Presence of additional aromatic ring and m-hydroxy substitution on that ring increases inhibitory activity. Space modeling study further adjudged the presence of hydrogen bond acceptor, hydrophobic and aromatic ring and critical distance among features for the inhibitory activity.
Poster
Detection of Tyrosine Kinase Activity Using the PHERAstar
Tyrosine kinases are important regulators in cellular processes. Kinases have been found to be involved in diseases such as cancer and cardiovascular, therefore, molecules that modulate kinase function are expected to be promising new drug targets. In this poster, we will describe the performance of an AlphaScreen™ (amplified luminescent proximity homogeneous assay) tyrosine kinase assay on BMG LABTECH´s PHERAstar using an AlphaScreen™ specific excitation LASER.
Poster
Solid Phase Synthesis of a Fluorescent Peptide: Comparison of Fmoc-Lys(5-FAM)-Resin and Fmoc-Lys[5-FAM(Trt)-Resin
We have prepared and performed comparison studies using two kinds of resins, Fmoc-Lys(5-FAM)-Rink Amide resin (I) and Fmoc-Lys[5-FAM(trt)]-Rink Amide resin (II), the latter contains a phenolic hydroxyl group protected with a trityl group. Syntheses were carried out under the same standard conditions and the peptides obtained showed no significant difference in purity. The results of these studies showed that resin (I) is adequate for synthesis of C-terminal fluorescent labeled peptide.
Poster
The Impact of the PCK1 Gene and PPCK1 Promoter Polymorphism 232C→G on the Incidence of TIIDM in Oji-Cree Natives of Ontario
The reported incidence of Type II Diabetes Mellitus (TIIDM) in Oji-Cree Natives is the highest in the world. This poster presents the impact of the PCK1 gene on TIIDM incidence in Oji-Cree Natives with particular attention to the role of SNP 232C→G on the transcription rate of phosphoenolpyruvate carboxykinease (PPCK1).
Poster
EM Algorithm for Gene Copy Number Estimation Using TaqMan® Assays
Recently, TaqMan® assays have been developed for detection of genetic variation at gene level using primers and probes designed for genomic DNA sequences. The R package TaqGCN contains classes and methods that can be used for data reading and plotting, and for predicting gene copy number.
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