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Molecules 2015, 20(1), 573-594;

Halofuginone — The Multifaceted Molecule

The Volcani Center, Institute of Animal Science, P.O. Box 6, Bet Dagan 50250, Israel
Department of Animal Sciences, Hebrew University of Jerusalem, Rehovot 76100, Israel
Author to whom correspondence should be addressed.
Academic Editor: Isabel C. F. R. Ferreira
Received: 8 December 2014 / Accepted: 25 December 2014 / Published: 5 January 2015
(This article belongs to the Collection Bioactive Compounds)
Full-Text   |   PDF [3080 KB, uploaded 5 January 2015]   |  


Halofuginone is an analog of febrifugine—an alkaloid originally isolated from the plant Dichroa febrifuga. During recent years, halofuginone has attracted much attention because of its wide range of beneficial biological activities, which encompass malaria, cancer, and fibrosis-related and autoimmune diseases. At present two modes of halofuginone actions have been described: (1) Inhibition of Smad3 phosphorylation downstream of the TGFβ signaling pathway results in inhibition of fibroblasts-to-myofibroblasts transition and fibrosis. (2) Inhibition of prolyl-tRNA synthetase (ProRS) activity in the blood stage of malaria and inhibition of Th17 cell differentiation thereby inhibiting inflammation and the autoimmune reaction by activation of the amino acid starvation and integrated stress responses. This review deals with the history and origin of this natural product, its synthesis, its known modes of action, and it’s various biological activities in pre-clinical animal models and in humans. View Full-Text
Keywords: malaria; fibrosis; inflammation; autoimmunity; Th-17; apoptosis malaria; fibrosis; inflammation; autoimmunity; Th-17; apoptosis

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Pines, M.; Spector, I. Halofuginone — The Multifaceted Molecule. Molecules 2015, 20, 573-594.

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