Department of Chemistry and Chemical Biology and Department of Biochemistry and Biomedical Sciences, M. G. DeGroote Institute for Infectious Disease Research, McMaster University, 1280 Main Street West, Hamilton, Ontario, L8N 3Z5, Canada.
Chembiochem. 2013 Mar 4;14(4):431-5. doi: 10.1002/cbic.201200598. Epub 2013 Feb 10.
Natural lipocyclocarbamate natural products have provided the inspiration for the first-in-class synthetic phospholipase inhibitor darapladib, currently in phase III clinical trials for the treatment of atherosclerosis. Here, we discuss their biosynthesis by a nonribosomal peptide synthetase.
天然脂环碳酸酯天然产物为首个合成的磷脂酶抑制剂达拉普利的设计提供了灵感,目前正在进行治疗动脉粥样硬化的 III 期临床试验。在这里,我们讨论了它们由非核糖体肽合成酶合成的过程。