Abstract
To exploit natural products as a source of biologically active compounds, accelerating the discovery of analogues that exhibit more potent and modulated biological activities is essential. In this chapter, two specific examples of a one-bead-one-compound (OBOC)-based functional enhancement and modulation of peptidic natural products are demonstrated. As structurally distinct natural product scaffolds, macrocyclic lysocin E and linear gramicidin A were adopted. The combination of solid-phase synthesis with a split-and-mix approach, microscale functional evaluation, and structure determination based on tandem mass spectrometry led to the successful discovery of natural product analogues that exhibited enhanced and altered functions. These results exemplify the potential of this strategy for accelerating the structure–activity relationship study and structural optimization of natural products.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
