A novel biochemical assay has been developed to rapidly and sensitively screen for antagonist compounds targeting aldolase A (ALDOA), a key enzyme in cancer cell metabolism. The optimized assay is high-throughput friendly, cost- and labor-efficient, and suitable for analysis of multiple NADH-dependent enzymes.
A new methodology for correlating compound identity to CYP1A2 potency of inhibitors in metabolic mixtures has been developed, providing direct identification of compounds with inhibitory properties. This approach allows for rapid assessment of pharmacokinetic properties of drugs and their metabolites, improving drug development.
A new homogeneous assay detects succinate using luminescence, enabling the investigation of a large number of structurally conserved enzymes belonging to the Fe(II)/2-oxoglutarate-dependent dioxygenase superfamily. This method has significant applications in dioxygenase research and has the potential to impact human diseases.
This special issue highlights innovations in MALDI mass spectrometry for characterizing proteomes, detecting analytes, and screening non-covalent binding of small molecules to target proteins. MALDI imaging is used to study diseases and therapeutics, including the distribution of glycosphingolipids in a Gaucher Disease model mouse brain.
Self-reporting theranostic nanoparticles can provide real-time disease monitoring and tracking. The emerging field of responsive theranostic nanoparticles has the potential to advance imaging platforms and improve disease diagnosis.
A new technology bridges clinical pathology assessment, high-content analysis, and 3D cell cultures, allowing rapid, automatable, and multiplex readouts. This technique is applied to mixed arrays made up of spheroid models from various cell lines, demonstrating its potential for safety and efficacy testing and model optimization.
The article explores how automation and innovative screens are influencing the search for inhibitors and activators of protein tyrosine phosphatases, which have been implicated in many human diseases. The resulting compounds are facilitating exploration of fundamental cellular processes controlled by phosphatases in cancers.
Researchers discuss evolving treatments and future therapies for osteoarthritis pain, highlighting the limitations of existing treatments and introducing new potential treatment targets. Combination therapies and biomarkers are also explored as promising approaches to improve effective pain treatment.
This special issue reports advancements in assay design, microfluidic technologies, and digital assays for improved quantification of rare mutations, molecular analysis, and mechanobiological studies. It also highlights improvements in tissue dissection and sample processing for cancer diagnostics and drug screening.
The unfolded protein response (UPR) is an adaptive biochemical process linked to cell homeostasis, crucial for maintaining normal physiological function. Prolonged ER stress can push the UPR past beneficial functions, contributing to various disease states, making it a global target for novel therapeutic intervention.