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Drug Affinity Responsive Target Stability (DARTS) Identifies Laurifolioside as a New Clathrin Heavy Chain Modulator | |
Dal Piaz, F; Saltos, MBV; Franceschelli, S; Forte, G; Marzocco, S; Tuccinard, T; Poli, G; Ebrahimi, SN; Hamburger, M; De Tommasi, N; Braca, A | |
2016 | |
Source Publication | JOURNAL OF NATURAL PRODUCTS
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ISSN | 0163-3864 |
Volume | 79Issue:10Pages:2681-2692 |
Abstract | Five new diterpenes (1-5) and a megastigmane derivative (6) were isolated from the aerial parts of Euphorbia laurifolia, along with several known compounds. Their structures were elucidated by NMR, MS, and ECD and by chemical methods. A chemical proteomics drug affinity responsive target stability (DARTS) approach to investigate the lathyrane diterpene 1, laurifolioside, on its putative cellular target(s) was performed. Clathrin heavy chain 1, a protein mainly involved in selective uptake of proteins, viruses, and other macromolecules at the plasma membrane of cells, was identified as the major interaction partner of compound 1. The modulation of clathrin activity by 1 was studied through microscopy, molecular docking, and molecular dynamics studies, suggesting a new activity of lathyrane diterpenes in the modulation of trafficking pathways. |
Keyword | Macrocyclic Diterpenes Lathyrane Diterpenes Multidrug-resistance Euphorbia Hsp90 Latex Cells |
Indexed By | WOS:000386745300032 |
Language | 英语 |
Document Type | 期刊论文 |
Identifier | https://ir.xtbg.ac.cn/handle/353005/10213 |
Collection | 文献共享 |
Recommended Citation GB/T 7714 | Dal Piaz, F,Saltos, MBV,Franceschelli, S,et al. Drug Affinity Responsive Target Stability (DARTS) Identifies Laurifolioside as a New Clathrin Heavy Chain Modulator[J]. JOURNAL OF NATURAL PRODUCTS,2016,79(10):2681-2692. |
APA | Dal Piaz, F.,Saltos, MBV.,Franceschelli, S.,Forte, G.,Marzocco, S.,...&Braca, A.(2016).Drug Affinity Responsive Target Stability (DARTS) Identifies Laurifolioside as a New Clathrin Heavy Chain Modulator.JOURNAL OF NATURAL PRODUCTS,79(10),2681-2692. |
MLA | Dal Piaz, F,et al."Drug Affinity Responsive Target Stability (DARTS) Identifies Laurifolioside as a New Clathrin Heavy Chain Modulator".JOURNAL OF NATURAL PRODUCTS 79.10(2016):2681-2692. |
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