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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 PublicationJOURNAL OF NATURAL PRODUCTS
ISSN0163-3864
Volume79Issue:10Pages:2681-2692
AbstractFive 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.
KeywordMacrocyclic Diterpenes Lathyrane Diterpenes Multidrug-resistance Euphorbia Hsp90 Latex Cells
Indexed ByWOS:000386745300032
Language英语
Document Type期刊论文
Identifierhttp://ir.xtbg.org.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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