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Analysis of receptor-ligand binding by photoaffinity cross-linking

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Abstract

Photoaffinity cross-linking is a fast developing technology for biomolecular interactions, including receptor-ligand binding. The chemical mechanisms of the most commonly used photoactivatable probes and their respective photochemistry are summarized. This review focuses on the expanding utilities of this technology as a result of recent advances in the (i) identification of receptor contact sites, (ii) monitoring ligand-induced receptor conformational changes, (iii) identification of global binding surfaces, (iv) binding mode analysis using bifunctional photo-probes, (v) application of biosynthetic photo-probes, and (vi) examples of novel target discovery using this technology. Limitations and future potential of this approach are also discussed.

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Authors and Affiliations

  1. Department of Biochemistry and Center for Drug Discovery, Virginia Tech, Blacksburg, VA, 24061, USA

    Bin Xu & Ling Wu

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  1. Bin Xu
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  2. Ling Wu
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Correspondence to Bin Xu.

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Xu, B., Wu, L. Analysis of receptor-ligand binding by photoaffinity cross-linking. Sci. China Chem. 57, 232–242 (2014). https://doi.org/10.1007/s11426-013-5045-z

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  • DOI: https://doi.org/10.1007/s11426-013-5045-z

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