Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, College of Chemical Engineering, Nanjing Forestry University, Nanjing, China.
Department of Biological Engineering, Graduate School of Science and Engineering, Yamagata University, Yonezawa, Japan.
Chirality. 2022 Jan;34(1):86-103. doi: 10.1002/chir.23376. Epub 2021 Oct 29.
Amino acids (AAs) play an important role in the modern health industry as key synthetic precursors for pharmaceuticals, biomaterials, biosensors, and drug delivery systems. Currently, over 30% of small-molecule drugs contain residues of tailor-made AAs or derived from them amino-alcohols and di-amines. In this review article, we profile 12 AA-derived new pharmaceuticals approved by the FDA in 2020. These newly introduced drugs include Tazverik (epithelioid sarcoma), Gemtesa (overactive bladder), Zeposia (multiple sclerosis), Byfavo (induction and maintenance of procedural sedation), Cu 64 dotatate, and Gallium 68 PSMA-11 (both PET imaging), Rimegepant (acute migraine), Zepzelca (lung cancer), Remdesivir (COVID-19), Amisulpride (nausea and vomiting), Setmelanotide (obesity), and Lonafarnib (progeria syndrome). For each compound, we describe the spectrum of biological activity, medicinal chemistry discovery, and synthetic preparation.
氨基酸（AAs）在现代健康产业中发挥着重要作用，是制药、生物材料、生物传感器和药物输送系统的关键合成前体。目前，超过 30%的小分子药物含有定制氨基酸或衍生自它们的氨基酸-醇和二胺残基。在这篇综述文章中，我们介绍了 2020 年美国食品和药物管理局（FDA）批准的 12 种由氨基酸衍生的新药。这些新引入的药物包括 Tazverik（上皮样肉瘤）、Gemtesa（膀胱过度活动症）、Zeposia（多发性硬化症）、Byfavo（诱导和维持程序镇静）、Cu 64 dotatate 和 Gallium 68 PSMA-11（均为 PET 成像）、rimegepant（急性偏头痛）、Zepzelca（肺癌）、Remdesivir（COVID-19）、amisulpride（恶心和呕吐）、setmelanotide（肥胖症）和 lonafarnib（早衰综合征）。对于每种化合物，我们描述了其生物活性、药物化学发现和合成制备的范围。
