Multiwavelength Collisional Quenching to Study Ligand Protein Interactions in Glutamate Dehydrogenase

Hyperpolarized Water to Study Protein-Ligand Interactions.

The affinity between a chosen target protein and small molecules is a key aspect of drug discovery. Screening by popular NMR methods such as Water-LOGSY suffers from low sensitivity and from false positives caused by aggregated or denatured proteins. This work demonstrates that the sensitivity of Water-LOGSY can be greatly boosted by injecting hyperpolarized water into solutions of proteins and...

Quantifying Water-Mediated Protein–Ligand Interactions in a Glutamate Receptor: A DFT Study

It is becoming increasingly clear that careful treatment of water molecules in ligand-protein interactions is required in many cases if the correct binding pose is to be identified in molecular docking. Water can form complex bridging networks and can play a critical role in dictating the binding mode of ligands. A particularly striking example of this can be found in the ionotropic glutamate r...

Evaluation of Glutamate Dehydrogenase Activity and Insulin Secretion in Mice Exposed to Dexamethasone

Background and Aims: Diabetes is one of the most important endocrine disrupters and is associated with various hormones, including those that can lead to diabetes. Glucocorticoid use may lead to insulin resistance. Dexamethasone is one of these glucocorticoid compounds. Glutamate dehydrogenase plays a key role in the production of glutamate in the secretion of insulin. Based on these hormonal i...

Exploiting Ligand-Protein Conjugates to Monitor Ligand-Receptor Interactions

We introduce three assays for analyzing ligand-receptor interactions based on the specific conjugation of ligands to SNAP-tag fusion proteins. Conjugation of ligands to different SNAP-tag fusions permits the validation of suspected interactions in cell extracts and fixed cells as well as the establishment of high-throughput assays. The different assays allow the analysis of strong and weak inte...

Protein Ligand Interactions