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Experimental Methods Used for Identifying Small-Molecule Inhibitors of Protein-Protein Interaction

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Targeting Protein-Protein Interactions by Small Molecules

Abstract

Protein-protein interactions (PPIs) are implicated innumerous biological processes under physiological and pathophysiological conditions. They thus offer new opportunities for therapeutic intervention. Various experimental methods have been applied to the identification of small-molecule inhibitors targeting PPIs, which can be classified as biophysical, biochemical, and genetic methods. This chapter gives an overview of some widely applied experimental methods in each category, highlighting their principles, advantages, and disadvantages, as well as their recent developments.

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Acknowledgements

The authors are grateful for the financial supports from the National Natural Science Foundation of China (Grant No. 81430083, 21472227, 21673276 to Prof. R. Wang), the Ministry of Science and Technology of China (National Key R&D Program of China Grant No. 2016YFA0502302 to Prof. R. Wang), Chinese Academy of Sciences (Strategic Priority Research Program, Grant No. XDB20000000, No. XDB20020200), and the Science and Technology Development Foundation of Macao SAR (Grant No. 055/2013/A2 to Prof. R. Wang).

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  1. State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032, People’s Republic of China

    Mi Zhou, Qing Li, Wenna Kong & Renxiao Wang

  2. State Key Laboratory of Quality Research in Chinese Medicine, Macau Institute for Applied Research in Medicine and Health, Macau University of Science and Technology, Macau, People’s Republic of China

    Renxiao Wang

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Correspondence to Renxiao Wang .

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  1. School of Pharmacy, Second Military Medical University, Shanghai, China

    Chunquan Sheng

  2. College of Pharmacy, University of Minnesota, Minneapolis, Minnesota, USA

    Gunda I. Georg

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Zhou, M., Li, Q., Kong, W., Wang, R. (2018). Experimental Methods Used for Identifying Small-Molecule Inhibitors of Protein-Protein Interaction. In: Sheng, C., Georg, G. (eds) Targeting Protein-Protein Interactions by Small Molecules. Springer, Singapore. https://doi.org/10.1007/978-981-13-0773-7_5

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