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Drug affinity responsive target stability (DARTS) identifies laurifolioside as a new clathrin heavy chain modulator

Dal Piaz, F. and Vera Saltos, M. B. and Franceschelli, S. and Forte, G. and Marzocco, S. and Tuccinardi, T. and Poli, G. and Ebrahimi, S. N. and Hamburger, M. and De Tommasi, N. and Braca, A.. (2016) Drug affinity responsive target stability (DARTS) identifies laurifolioside as a new clathrin heavy chain modulator. Journal of Natural Products, 79 (10). pp. 2681-2692.

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Official URL: http://edoc.unibas.ch/52794/

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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.
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Pharmazeutische Biologie (Hamburger)
UniBasel Contributors:Hamburger, Matthias
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:American Chemical Society
ISSN:0163-3864
e-ISSN:1520-6025
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:30 Oct 2017 08:24
Deposited On:30 Oct 2017 08:24

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