Identification of non-peptidic neuromedin U receptor modulators by a robust homogeneous screening assay

Screening Assay for Selective Estrogen Receptor Modulators

Identification and functional characterization of a novel subtype of neuromedin U receptor.

Neuromedin U is a bioactive peptide isolated originally from the porcine spinal cord. We recently identified neuromedin U as the cognate ligand for the orphan G protein-coupled receptor FM-3. In this study, we isolated cDNA coding for a novel G protein-coupled receptor, TGR-1, which was highly homologous with FM-3. We found that neuromedin U specifically and clearly elevated the extracellular a...

Detection of thymidylate synthase modulators by a novel screening assay.

Thymidylate synthase (TS), a key cancer chemotherapeutic target, catalyzes the conversion of deoxyuridylate to thymidylate. TS can serve as a repressor of its own synthesis by binding to its own mRNA through TS-specific binding elements (TBEs). In this report, we describe the use of a luciferase reporter plasmid containing two TBEs that can be used as a tool for the identification and initial p...

Non-peptidic Cruzain Inhibitors with Trypanocidal Activity Discovered by Virtual Screening and In Vitro Assay

A multi-step cascade strategy using integrated ligand- and target-based virtual screening methods was developed to select a small number of compounds from the ZINC database to be evaluated for trypanocidal activity. Winnowing the database to 23 selected compounds, 12 non-covalent binding cruzain inhibitors with affinity values (K i) in the low micromolar range (3-60 µM) acting through a competi...

Research resource: modulators of glucocorticoid receptor activity identified by a new high-throughput screening assay.

Glucocorticoid steroids affect almost every type of tissue and thus are widely used to treat a variety of human pathological conditions. However, the severity of numerous side effects limits the frequency and duration of glucocorticoid treatments. Of the numerous approaches to control off-target responses to glucocorticoids, small molecules and pharmaceuticals offer several advantages. Here we ...