A novel strategy for site selective spin-labeling to investigate bioactive entities by DNP and EPR spectroscopy.

ABSTRACT: A novel specific spin-labeling strategy for bioactive molecules is presented for eptifibatide (integrilin) an antiplatelet aggregation inhibitor, which derives from the venom of certain rattlesnakes. By specifically labeling the disulfide bridge this molecule becomes accessible for analytical techniques such as Electron Paramagnetic Resonance (EPR) and solid state Dynamic Nuclear Polarization (DNP). The necessary spin-label was synthesized and inserted into the disulfide bridge of eptifibatide via reductive followed by insertion by a double Michael addition under physiological conditions. This procedure is universally applicable for disulfide containing biomolecules and is expected to preserve their tertiary structure with minimal change due to the small size of the label and restoring of

SUBMITTER: Herr K 

PROVIDER: S-EPMC8249612 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature