Using photolabile ligands in drug discovery and development

Photoactivatable ligands are important tools used in drug discovery and drug development. These ligands enable researchers to identify the targets of durgs, to determine the affinity and selectivity of the drug–target interaction, and to identify the binding site on the target. Examples are presented from three fundamentally different approaches: (1) photoaffinity labeling of target macromolecules; (2) photoactivation and release of ‘caged ligandsʹ; and (3) photoimmobilization of ligands onto surfaces.