Kinome chemoproteomics characterization of pyrrolo[3,4-c]pyrazoles as potent and selective inhibitors of glycogen synthase kinase 3.

Glycogen synthase kinase 3 has evolutionarily conserved roles in cell signaling and metabolism and is a recognized drug target in neurological pathologies, most prominently bipolar disorder. More recently it has been suggested that GSK3 may be a target for the treatment of trypanosomatid parasite infections, e.g.

Development of a Cotton Smart Textile with Medicinal Properties Using Lime Oil Microcapsules.

The present study focused on using microencapsulation technique to develop an antioxidant and antibacterial active smart cotton fabric using encapsulated lime oil (LO). LO microcapsules were prepared via the complex coacervation method using chitosan and gum arabic wall materials. UV-Visible and FTIR spectrometry verified the successful encapsulation of LO.

Rapid profiling of protein kinase inhibitors by quantitative proteomics.

The ability to determine structure-activity relationships (SAR) and identify cellular targets from cell lysates and tissues is of great utility for kinase inhibitor drug discovery. We describe a streamlined mass spectrometry-based chemoproteomics workflow to examine the SAR and target profiles of a small library of kinase inhibitors that consists of the drug dasatinib and a panel of general type II inhibitors. By combining a simplified affinity enrichment and on-bead protein digestion workflow with quantitative proteomics, we achieved sensitive and specific enrichment of target kinases using our small molecule probes.