Literature DB >> 30160121

Biemamides A-E, Inhibitors of the TGF-β Pathway That Block the Epithelial to Mesenchymal Transition.

Fan Zhang1, Doug R Braun1, Gene E Ananiev2, F Michael Hoffmann3, I-Wei Tsai1, Scott R Rajski1, Tim S Bugni1.   

Abstract

Screening of a marine natural products library for inhibitors of TGF-β revealed five pyrimidinedione derivatives, biemamides A-E (1-5). The structures were determined by 2D NMR and HRMS experiments; absolute configurations were established by advanced Marfey's analysis and ECD calculations. Biemamides A-E specifically inhibited in vitro TGF-β induced epithelial to mesenchymal transition in NMuMG cells. Additionally, using Caenorhabditis elegans, selected biemmamides were found to influence in vivo developmental processes related to body size regulation in a dose-dependent manner.

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Year:  2018        PMID： 30160121      PMCID： PMC6207949          DOI： 10.1021/acs.orglett.8b01871

Source DB:  PubMed          Journal:  Org Lett        ISSN： 1523-7052            Impact factor:   6.005


  26 in total

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