|Some thiazole derivatives as potent antiproliferative agents with CDK2/Cycin E/A inhibitory activities|
Mahesh Chhabria1, Shailesh Patel*1, Maulik Suthar2
We report synthesis and biological evaluation of novel thiazole derivatives. High throughput screening of various compounds for their anti-proliferative activity led to the identification of thiazolo-thiones as potential candidate for Lung cancer (NCl-H23, NClH510A, NCI-H522) and breast cancer (MDA-MB-453/231/468, MCF-7). The most potent compounds were also screened for their inhibitory activity against CDK2/ Cyclin E/A which are considered as promising targets for lung and breast cancer.
|Predicting hepatotoxicity: Reactive metabolite trapping using glutathione and freshly isolated hepatocytes|
Birks, V., Webber, G., Geoffroy, S., Cole, R., and Wood, S.
This poster presents our results to date using clozapine (a compound known to be associated with GSH-adduct formation) as substrate and using stable isotope GSH (GSH13C2,15N) to enhance specificity. In addition, all analyses have been conducted using an Waters Acquity UPLC-MS/MS. Results we have obtained in hepatocytes are compared against findings using human liver microsomes (HLM).
|A simple, fast and quantitative single-step dead-cell indicator for flow cytometry|
Jixiang Liu, Jolene Bradford, Chris Langsdorf
We have evaluated a series of new compounds for dead cell stain and identified a new product, SYTOX® AADvancedTM dead cell stain, which demonstrates improved properties over 7-AAD. These properties make the SYTOX® AADvancedTM dead cell stain a simple, fast and quantitative single-step no-wash dead-cell indicator as well as ideal for use in multicolor application requiring DNA content.
|Protein array-based screening of autoantibody signatures|
Zingaretti C., Arigò M., Colombatto P., Brunetto M., Muratori L., Bonino F., Bianchi F., Pagani M., De Francesco R., Abrignani S., Bombaci M.
The evidence for an association between autoimmune diseases and chronic HCV infection has been clearly established. To this aim, a protein array was employed to analyze serum samples of HCV patients w/wo autoimmune complications, of patients with autoimmune hepatitis but not infected with HCV and of healthy donors as controls. A panel of autoantigens able to discriminate among the three groups of patients was identified for potential use as biomarkers.
|PROTEOME WIDE PLASMA PROFILING USING ANTIBODY SUSPENSION BEAD ARRAYS|
Maja Neiman, Ulrika Igel, Burcu Ayoglu, Kimi Drobin, Mathias Uhlén, Peter Nilsson and Jochen M. Schwenk
A newly developed antibody suspension bead array assay allows for a systematic and high-throughput plasma profiling. This microtiter based assay uses antibody-coupled beads for a multiplexed analysis of minute amounts of directly labelled samples. The key requirement of a?nity reagents towards all human proteins is met by the Human Protein Atlas project.
|Five noncovalent peptidic ligands show different affinity rankings in solution and gas phase|
Andrey Dyachenko , Michael Goldflam , Marta Vilaseca , Ernest Giralt
Stability of noncovalent complexes of VEGF protein with 5 peptidic ligands is studied. Experiments were conducted in solution (NMR CSP, ITC) and in gas phase (CID TOF MS). Each ligand differs from others in chirality of one amino acid. It was shown, that trend of stability of the studied noncovalent complexes is reversed in the gas phase relatively to the solution. An explanation of this behavior is presented.
|Software for Genomic/Epigenomic Research|
A.S.Tanas, V.V.Shkarupo, E.B.Kuznetsova, D.V.Zaletayev, V.V. Strelnikov
We present two computer programs: 1) AIMS in silico - a suggestion tool for Amplification of Intermethylated Sites experimental design and results analysis; and 2) PeakPick – a tool to view & analyse capillary electrophoregrams Our computer software is intended to standardize AIMS applications and to turn it into one of the principal approaches towards cancer methylomes studies as well as towards diagnostics in oncology, including early screening.
|Insulin Decreases Transcription of Three Proteins Associated with Lung Surfactant|
Rucka, Z [a], Vanhara, P [b], Tesarova, L [a], Potesilova, M [a], Stejskal, S [a], Dolezel, J [c], Koutna, I [a]
Our project is partially focused on insulin affecting four proteins associated with lung surfactant. Small and hydrophobic SP-B and S-PC help to spread and stabilize the surfactant layer while large and hydrophilic SP-A and SP-D participate in immune responses. A549 and H441 cell lines were used. It was observed using RealTime PCR that higher doses of insulin lead to decreased transcription of SP-B, SP-C, SP-D, and both isoforms of SP-A.
|Synthesis and trafficking of the tonoplast potassium channel AtTPK1|
Marie Maitrejean (1,2), Michael Wudick (2), Camilla Voelker (2), Katrin Czempinski (2), Emanuela Pedrazzini (1), Alesandro Vitale (1)
Sorting signals of tonoplast proteins and the pathway they follow through the endomembrane system are still poorly characterized. Using Brefeldin A (an inhibitor of the Golgi-mediated traffic) we showed that a Golgi-dependent pathway for tonoplast delivery may exist. Then we generated various chimeric TPK1-TPK4 fusions, exchanging various domains. We observed that the cytosolic, C-terminal domain of TPK1 is sufficient to re-direct the plasma membrane TPK4 to the tonoplast.