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Target identification for biologically active small molecules using chemical biology approaches

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Abstract

The identification and validation of the targets of biologically active molecules is an important step in the field of chemical biology. While recent advances in proteomic and genomic technology have accelerated this identification process, the discovery of small molecule targets remains the most challenging step. A general method for the identification of these small molecule targets has not yet been established. To overcome the difficulty in target identification, new technology derived from the fields of genomics, proteomics, and bioinformatics has been developed. To date, pull-down methods using small molecules immobilized on a solid support followed by mass spectrometry have been the most successful approach. Here, we discuss current procedures for target identification. We also review the most recent target identification approaches and present several examples that illustrate advanced target identification technology.

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Acknowledgments

This work was supported by research fund of Korea institute of Science and Technology (2Z04371).

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Authors and Affiliations

  1. Department of Oral Anatomy, College of Dentistry, Gangneung Wonju National University, Gangneung, 210-340, Republic of Korea

    Heesu Lee

  2. Research Institute of Oral Science, Gangneung Wonju National University, Gangneung, 210-340, Republic of Korea

    Heesu Lee

  3. Natural Constituent Research Center, Korea Institute of Science and Technology, Gangneung, 210-340, Republic of Korea

    Jae Wook Lee

  4. Convergence Research Center for Dementia, Korea Institute of Science and Technology, Seoul, 210-340, Republic of Korea

    Jae Wook Lee

  5. Department of Biological Chemistry, Korea University of Science and Technology, Daejeon, Republic of Korea

    Jae Wook Lee

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  1. Heesu Lee
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Correspondence to Jae Wook Lee.

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Lee, H., Lee, J.W. Target identification for biologically active small molecules using chemical biology approaches. Arch. Pharm. Res. 39, 1193–1201 (2016). https://doi.org/10.1007/s12272-016-0791-z

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