DiMarchi Richard D, Mayer John P, Gelfanov Vasily M, Tschöp Matthias
Department of Chemistry, Indiana University, Bloomington, IN, 47405, USA.
Novo Nordisk Research Center Indianapolis, Indianapolis, IN, 46241, USA.
J Pept Sci. 2018 Jan;24(1). doi: 10.1002/psc.3056.
This review presents the scope of research presented in an October 2016 lecture pertaining to the award of the 2015 Max Bergmann Medal. The advancement in synthetic and biosynthetic chemistry as applied to the discovery of novel macromolecular drug candidates is reviewed. The evolution of the technology from the design, synthesis, and development of the first biosynthetic peptides through the emergence of peptide-based incretin agonists that function by multiple biological mechanisms is exemplified by the progression of such peptides from preclinical to clinical study. A closing section highlights recent progress made in total chemical synthesis of insulin and related peptides.
本综述介绍了2016年10月一场关于2015年马克斯·伯格曼奖章授予的讲座中所呈现的研究范围。对应用于新型大分子候选药物发现的合成化学和生物合成化学的进展进行了综述。从首个生物合成肽的设计、合成和开发，到通过多种生物学机制发挥作用的基于肽的肠促胰岛素激动剂的出现，该技术的演变以这类肽从临床前研究到临床研究的进展为例进行了说明。结尾部分重点介绍了胰岛素及相关肽全化学合成方面取得的最新进展。
