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OCTN Cation Transporters in Health and Disease: Role as Drug Targets and Assay Development 14 Aug 2013 | 03:46 am

The three members of the organic cation transporter novel subfamily are known to be involved in interactions with xenobiotic compounds. These proteins are characterized by 12 transmembrane segments co...

A Label-Free LC/MS/MS-Based Enzymatic Activity Assay for the Detection of Genuine Caspase Inhibitors and SAR Development 14 Aug 2013 | 03:46 am

The resurgence of interest in caspases (Csp) as therapeutic targets for the treatment of neurodegenerative diseases prompted us to examine the suitability of published nonpeptidic Csp-3 and Csp-6 inhi...

Development of LC/MS/MS, High-Throughput Enzymatic and Cellular Assays for the Characterization of Compounds That Inhibit Kynurenine Monooxygenase (KM... 14 Aug 2013 | 03:46 am

Kynurenine monooxygenase (KMO) catalyzes the conversion of kynurenine to 3-hydroxykynurenine. Modulation of KMO activity has been implicated in several neurodegenerative diseases, including Huntington...

Development of a Pharmacodynamic Assay Based on PLC{gamma}2 Phosphorylation for Quantifying Spleen Tyrosine Kinase (SYK)-Bruton's Tyrosine Kinase (BTK... 14 Aug 2013 | 03:46 am

Spleen tyrosine kinase (SYK) and Bruton’s tyrosine kinase (BTK) are key mediators in coupling cell surface receptors, such as the B-cell receptor (BCR), to downstream signaling events affecting divers...

Development of a Colorimetric and a Fluorescence Phosphatase-Inhibitor Assay Suitable for Drug Discovery Approaches 14 Aug 2013 | 03:46 am

Protein phosphatases (PP) are interesting drug targets. However, their ubiquitous presence and involvement in different, partially opposing signal pathways suggest that specificity may be achieved rat...

High-Throughput Screening AlphaScreen Assay for Identification of Small-Molecule Inhibitors of Ubiquitin E3 Ligase SCFSkp2-Cks1 14 Aug 2013 | 03:46 am

Decreased levels of cell cycle inhibitor p27Kip1 due to excessive degradation occur in a variety of aggressive human tumors. Since reduced p27Kip1 expression has been associated with a poor prognosis ...

Development of a Quantitative Assay Amenable for High-Throughput Screening to Target the Type II Secretion System for New Treatments against Plant-Pat... 14 Aug 2013 | 03:46 am

Plant-pathogenic bacteria are the causative agents of diseases in important agricultural crops and ornamental plants. The severe economic burden of these diseases requires seeking new approaches for t...

High-Throughput Screen for Pharmacoperones of the Vasopressin Type 2 Receptor 14 Aug 2013 | 03:46 am

Pharmacoperone drugs correct the folding of misfolded protein mutants and restore function (i.e., "rescue") by correcting the routing of (otherwise) misrouted mutants. Assays for pharmacoperones have ...

A Timetable Organizer for the Planning and Implementation of Screenings in Manual or Semi-Automation Mode 14 Aug 2013 | 03:46 am

We have designed an Excel spreadsheet to facilitate the planning and execution of screenings performed manually or in semi-automation mode, following a sequential set of events. Many assays involve mu...

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