Tandem photoaffinity labeling-bioorthogonal conjugation in medicinal chemistry.

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. Copyright © 2012 Elsevier Ltd. All rights reserved.

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David J Lapinsky. Tandem photoaffinity labeling-bioorthogonal conjugation in medicinal chemistry. Bioorganic & medicinal chemistry. 2012 Nov 1;20(21):6237-47

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PMID: 23026086

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