A Platform of Phenol-Based Nitroxide Radicals as an "EPR Toolbox" in Supramolecular and Click Chemistry.

A large number (63) of well-defined nitroxide radicals, all phenol-based TEMPO and PROXYL esters, were synthesized using different strategies based on well-established Steglich esterifications. All of these radicals can be used as spin probes (SPs) and spin labels (SLs) for electron paramagnetic resonance (EPR) spectroscopy of supramolecular systems. Depending on the nature of the functional group(s) on each SP/SL, the synthesized nitroxide radicals serve as polyphilic molecular "toolbox" for the EPR-spectroscopic detection and characterization of specific types of interactions, e.

Conjugation of Amine-Functionalized Polyesters With Dimethylcasein Using Microbial Transglutaminase.

Protein-polymer conjugates have been used as therapeutics because they exhibit frequently higher stability, prolonged in vivo half-life, and lower immunogenicity compared with native proteins. The first part of this report describes the enzymatic synthesis of poly(glycerol adipate) (PGA(M)) by transesterification between glycerol and dimethyl adipate using lipase B from Candida antarctica. PGA(M) is a hydrophilic, biodegradable but water insoluble polyester.

Characterizing Active Pharmaceutical Ingredient Binding to Human Serum Albumin by Spin-Labeling and EPR Spectroscopy.

Drug binding to human serum albumin (HSA) has been characterized by a spin-labeling and continuous-wave (CW) EPR spectroscopic approach. Specifically, the contribution of functional groups (FGs) in a compound on its albumin-binding capabilities is quantitatively described. Molecules from different drug classes are labeled with EPR-active nitroxide radicals (spin-labeled pharmaceuticals (SLPs)) and in a screening approach CW-EPR spectroscopy is used to investigate HSA binding under physiological conditions and at varying ratios of SLP to protein.