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Mid-Sized Macrocyclic Peptides as a New Drug Modality

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Middle Molecular Strategy

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Abstract

Even though peptides are a major class of therapeutics since the early twentieth century, they had been rather considered as an elusive modality due to their low proteolytic stability and poor membrane permeability. Recently, it has become increasingly evident that mid-sized macrocyclic peptides containing exotic building blocks could exhibit specific/strong binding to various protein targets. Particularly, recent advance in ribosomal construction of random peptide libraries and their selection-based screening has revolutionized the discovery process of such molecules. In this chapter, we comprehensively summarize the background of currently available technologies developed by our laboratory and their recent outcomes, and also disclose new emerging technologies for synthesis and screening of artificial macrocycles.

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Authors and Affiliations

  1. Department of Chemistry, Graduate School of Science, The University of Tokyo, Bunkyo, Tokyo, 113-0033, Japan

    Yuki Goto, Masanobu Nagano & Hiroaki Suga

Authors
  1. Yuki Goto
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  2. Masanobu Nagano
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  3. Hiroaki Suga
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Correspondence to Yuki Goto or Hiroaki Suga .

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Editors and Affiliations

  1. Graduate School of Science, Osaka University, Toyanaka, Osaka, Japan

    Koichi Fukase

  2. Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Japan

    Takayuki Doi

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Goto, Y., Nagano, M., Suga, H. (2021). Mid-Sized Macrocyclic Peptides as a New Drug Modality. In: Fukase, K., Doi, T. (eds) Middle Molecular Strategy. Springer, Singapore. https://doi.org/10.1007/978-981-16-2458-2_6

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