Abstract
The use of light-activated chemical probes to study biological interactions was first discovered in the 1960s, and has since found many applications in studying diseases and gaining deeper insight into various cellular mechanisms involving protein–protein, protein–nucleic acid, protein–ligand (drug, probe), and protein–co-factor interactions, among others. This technique, often referred to as photoaffinity labelling, uses radical precursors that react almost instantaneously to yield spatial and temporal information about the nature of the interaction and the interacting partner(s). This review focuses on the recent advances in chemical biology in the use of benzophenones and diazirines, two of the most commonly known light-activatable radical precursors, with a focus on the last three years, and is intended to provide a solid understanding of their chemical and biological principles and their applications.
Highlights
The use of radicals or photoactivatable radical precursors has become ubiquitous in the fields of medicinal chemistry and chemical biology in the past three decades
This review focuses on the chemistry of two commonly used photoreactive chemical groups (PCG), benzophenone and diazirines, as representatives of two classes of radical precursors (1,2-diradical and carbene radical, respectively; Scheme 1), and their applications in biological systems with an emphasis on the last three years
Initial efforts in the 1960s aimed at using carbene precursors such as diazoacetates for photoaffinity labelling (PL) [35] which were later superseded by phenyldiazirines and spiro-adamantane-2,20 -diazirine, as introduced by Bayley and Knowles in 1978 [36]
Summary
The use of radicals or photoactivatable radical precursors has become ubiquitous in the fields of medicinal chemistry and chemical biology in the past three decades. Their main application revolves around studying the interactions of biomolecule targets such as proteins with ligands containing photoactivatable handles. After a given incubation period of the photolabelled probe in the biological system, the probe can be activated by light to reveal its biomolecular interactions, providing spatial and temporal information. This technique is referred to as photoaffinity labelling (PL).
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
