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Peptidomimetics and Peptide-Based Blockbuster Drugs


Jianlin Han, Hiroyuki Konno, Tatsunori Sato, Kunisuke Izawa* and Vadim A. Soloshonok*  


Amino acids (AAs) play an important role in modern health industry. AAs’ residues are frequently found in the structures of small-molecule modern pharmaceuticals, while peptidomimetics and peptide-based drugs are entirely derived from AAs. The goal of this review article is to highlight that, currently, AAs serve as key structural features in numerous successful pharmaceuticals; they are the so-called blockbuster drugs. In this work, we provide a detailed profile of 5 peptidomimetics and 4 peptide drugs. For each compound, we describe the spectrum of biological activity, medicinal chemistry discovery, and synthetic preparation.


Tailor-made amino acids, blockbuster drugs, peptidomimetic, peptides, modern pharmaceuticals, drug design and development, asymmetric synthesis


Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, College of Chemical Engineering, Nanjing Forestry University, Nanjing 210037 Jiangsu, Department of Biological Engineering, Graduate School of Science and Engineering, Yamagata University, Yonezawa, Yamagata 992-8510, Hamari Chemical Ltd., 1-4-29 Kunijima, Higashi-Yodogawa-ku, Osaka 533-0024, Hamari Chemical Ltd., 1-4-29 Kunijima, Higashi-Yodogawa-ku, Osaka 533-0024, Department of Organic Chemistry I, Faculty of Chemistry, University of the Basque Country UPV/EHU, Paseo Manuel Lardizábal 3, 20018 San Sebastián

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