title: Tandem photoaffinity labeling-bioorthogonal conjugation in medicinal chemistry.
abstract: Photoaffinity labeling has a longstanding history as a powerful biochemical technique. However, photoaffinity labeling has significantly evolved over the past decade principally due to its coupling with bioorthogonal/click chemistry reactions. This review aims to highlight tandem photoaffinity labeling-bioorthogonal conjugation as a chemical approach in medicinal chemistry and chemical biology. In particular, recent examples of using this strategy for affinity-based protein profiling (AfBPP), drug target identification, binding ensemble profiling, studying endogenous biological molecules, and imaging applications will be presented. Additionally, recent advances in the development of 'all-in-one' compact moieties possessing a photoreactive group and clickable handle will be discussed.
authors.affiliation: Division of Pharmaceutical Sciences, Duquesne University Mylan School of Pharmacy, 600 Forbes Avenue, Pittsburgh, PA 15282, USA. lapinskyd@duq.edu
authors.forename: David J
authors.initials: DJ
authors.lastname: Lapinsky
mesh_terms: D002626:Chemistry, Pharmaceutical; D057930:Click Chemistry; D019920:Photoaffinity Labels
chemical_list: D019920:Photoaffinity Labels