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Structure-activity-distribution relationship study of anti-cancer antimycin-type depsipeptides.

ABSTRACT: Small-molecule natural products have been an essential source of pharmaceuticals to treat human diseases, but very little is known about their behavior inside dynamic, live human cells. Here, we demonstrate the first structure-activity-distribution relationship (SADR) study of complex natural products, the anti-cancer antimycin-type depsipeptides, using the emerging bioorthogonal Stimulated Raman Scattering (SRS) Microscopy. Our results show that the intracellular enrichment and distribution of these compounds are driven by their potency and specific protein targets, as well as the lipophilic nature of compounds.

SUBMITTER: Seidel J

PROVIDER: S-EPMC6675640 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature

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Structure-activity-distribution relationship study of anti-cancer antimycin-type depsipeptides.

Seidel Jeremy J Miao Yupeng Y Porterfield William W Cai Wenlong W Zhu Xuejun X Kim Seong-Jong SJ Hu Fanghao F Bhattarai-Kline Santi S Min Wei W Zhang Wenjun W

Chemical communications (Cambridge, England) 20190801 63

Small-molecule natural products have been an essential source of pharmaceuticals to treat human diseases, but very little is known about their behavior inside dynamic, live human cells. Here, we demonstrate the first structure-activity-distribution relationship (SADR) study of complex natural products, the anti-cancer antimycin-type depsipeptides, using the emerging bioorthogonal Stimulated Raman Scattering (SRS) Microscopy. Our results show that the intracellular enrichment and distribution of ...[more]

PMID: 31317975

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