Department of Chemistry, Graduate School of Science, The University of Tokyo, 7-3-1 Bunkyo-ku, Tokyo 113-0033, Japan.
Chemistry. 2013 May 17;19(21):6530-6. doi: 10.1002/chem.201300247. Epub 2013 Mar 20.
Noncanonical peptides occur frequently in Nature, and often display high bioactivity. However, the lack of tractable systems for the synthesis of diverse libraries of such peptides has thus far hampered their development as drugs. Genetic reprogramming techniques, in which noncanonical amino acids may be incorporated into peptides, have largely removed this limitation. This Concept article outlines the development of these techniques with an emphasis on drug discovery.
非canonical 肽在自然界中频繁出现,并且通常具有很高的生物活性。然而,由于缺乏可用于合成多样化此类肽文库的可行系统,它们在药物开发方面受到了阻碍。遗传重编程技术可以将非canonical 氨基酸掺入到肽中,在很大程度上消除了这一限制。本文概念性地概述了这些技术的发展,并重点介绍了它们在药物发现方面的应用。