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Review | Regular issue | Vol 89, No. 12, 2014, pp.2697-2727
Published online, 14th November, 2014
DOI: 10.3987/REV-14-803
Diazirine-Based Multifunctional Photo-Probes for Affinity-Based Elucidation of Protein-Ligand Interaction

Takenori Tomohiro* and Yasumaru Hatanaka

*Graduate School of Medicines and Pharmaceutical Sciences for Research, Toyama University, 2630 Sugitani, Toyama, Toyama 930-0194, Japan


Diazirine-based photoaffinity labeling is recognized as one of the most reliable methods for analyzing protein-ligand interactions. Despite its excellent chemical and physical properties, the labeling process consists of an inefficient series of analytical steps: probe preparation, detection and isolation of the target protein, and identification of the labeled site within the active site. Firstly, this review introduces a versatile method for derivatization of trifluoromethylphenyldiazirine, the most common photocross-linker, then discusses its use in optimizing the probe for the simplification of labeled protein analyses including selective detection and purification, and the resulting acceleration of target protein identification by structural analysis. The present review reflects recent achievements in the chemistry and biological application of diazirine photoaffinity probes.