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Tools and rules for macrocycles

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The application of macrocycles to previously undruggable targets has aroused a great deal of interest in this structural class. Recent studies advance our understanding of the way macrocycles bind protein targets and provide new strategies and tools to generate peptide-based macrocycles.

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Figure 1: Development of macrocycle drugs.
Figure 2: Cyclization of peptides with butelase 1.

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Authors and Affiliations

  1. Christian Heinis is in the Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne, Switzerland.,

    Christian Heinis

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  1. Christian Heinis
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Correspondence to Christian Heinis.

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Heinis, C. Tools and rules for macrocycles. Nat Chem Biol 10, 696–698 (2014). https://doi.org/10.1038/nchembio.1605

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