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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
Chemical Compound Review

Halofuginone     7-bromo-6-chloro-3-[3-[(3R)- 3-hydroxy-2...

Synonyms: SureCN12996241, AC1L1XZM, C16H17BrClN3O3, LS-140372, AKOS015918193, ...
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Disease relevance of Halofuginone

  • Halofuginone given orally before fibrosis induction prevented the activation of most of the stellate cells and the remaining cells expressed low levels of collagen alpha1(I) gene, resulting in low levels of collagen [1].
  • These results suggest that halofuginone may become an effective and novel mode of therapy in the treatment of liver fibrosis [1].
  • Halofuginone also effectively suppresses tumor progression and metastasis in mice [2].
  • The ability of halofuginone to interfere with key events in neovascularization, together with its oral bioavailability and safe use as an anti-parasitic agent, make it a promising drug for further evaluation in the treatment of a wide range of diseases associated with pathological angiogenesis [2].
  • Halofuginone treatment alone exerted no toxicity but significantly lessened radiation-induced fibrosis [3].

High impact information on Halofuginone

  • Halofuginone inhibited the proliferation of other cell types of the fibrotic liver in vivo and inhibited collagen production and collagen alpha1(I) gene expression in the SV40-immortalized rat HSC-T6 cells in vitro [1].
  • These results together with the well-documented role of extracellular matrix (ECM) components and matrix degrading enzymes in formation of new blood vessels led us to investigate the effect of halofuginone on the angiogenic process [2].
  • The most conclusive anti-angiogenic activity of halofuginone was demonstrated in vivo (mouse corneal micropocket assay) by showing a marked inhibition of basic fibroblast growth factor (bFGF) -induced neovascularization in response to systemic administration of halofuginone, either i.p. or in the diet [2].
  • Halofuginone also suppresses extracellular matrix deposition and cell proliferation [4].
  • We have previously demonstrated that halofuginone, a widely used alkaloid coccidiostat, is a potent inhibitor of collagen alpha1(I) and matrix metalloproteinase 2 gene expression [4].

Chemical compound and disease context of Halofuginone


Biological context of Halofuginone


Anatomical context of Halofuginone


Associations of Halofuginone with other chemical compounds


Gene context of Halofuginone

  • The results detail the molecular effects of halofuginone on the TGF-beta signal pathway and show that halofuginone may lessen radiation-induced fibrosis in humans [3].
  • Because von Hippel-Lindau (VHL)-associated tumors express high levels of VEGF, it was of interest to ascertain the potential usefulness of halofuginone for treatment of these tumors [17].
  • Additionally, inhibition of Smad3 by overexpression of the inhibitory Smad7 protein or by treatment with the small molecule, halofuginone, dramatically reduces responses in animal models of kidney, lung, liver and radiation-induced fibrosis [18].
  • Halofuginone inhibits NF-kappaB and p38 MAPK in activated T cells [12].
  • CONCLUSION: Our findings illustrate the powerful down-regulatory property of c-Jun toward type I collagen and establish that halofuginone exerts its effect on collagen synthesis in a c-Jun-dependent manner [10].

Analytical, diagnostic and therapeutic context of Halofuginone


  1. Halofuginone to prevent and treat thioacetamide-induced liver fibrosis in rats. Bruck, R., Genina, O., Aeed, H., Alexiev, R., Nagler, A., Avni, Y., Pines, M. Hepatology (2001) [Pubmed]
  2. Halofuginone: a potent inhibitor of critical steps in angiogenesis progression. Elkin, M., Miao, H.Q., Nagler, A., Aingorn, E., Reich, R., Hemo, I., Dou, H.L., Pines, M., Vlodavsky, I. FASEB J. (2000) [Pubmed]
  3. Amelioration of radiation-induced fibrosis: inhibition of transforming growth factor-beta signaling by halofuginone. Xavier, S., Piek, E., Fujii, M., Javelaud, D., Mauviel, A., Flanders, K.C., Samuni, A.M., Felici, A., Reiss, M., Yarkoni, S., Sowers, A., Mitchell, J.B., Roberts, A.B., Russo, A. J. Biol. Chem. (2004) [Pubmed]
  4. Inhibition of bladder carcinoma angiogenesis, stromal support, and tumor growth by halofuginone. Elkin, M., Ariel, I., Miao, H.Q., Nagler, A., Pines, M., de-Groot, N., Hochberg, A., Vlodavsky, I. Cancer Res. (1999) [Pubmed]
  5. Reduction in pulmonary fibrosis in vivo by halofuginone. Nagler, A., Firman, N., Feferman, R., Cotev, S., Pines, M., Shoshan, S. Am. J. Respir. Crit. Care Med. (1996) [Pubmed]
  6. The effect of halofuginone lactate on experimental Cryptosporidium parvum infections in calves. Naciri, M., Mancassola, R., Yvoré, P., Peeters, J.E. Vet. Parasitol. (1993) [Pubmed]
  7. Screening for the coccidiostats halofuginone and nicarbazin in egg and chicken muscle: development of an ELISA. Huet, A.C., Mortier, L., Daeseleire, E., Fodey, T., Elliott, C., Delahaut, P. Food additives and contaminants. (2005) [Pubmed]
  8. Prevalence and control of bovine cryptosporidiosis in German dairy herds. Joachim, A., Krull, T., Schwarzkopf, J., Daugschies, A. Vet. Parasitol. (2003) [Pubmed]
  9. Field study of the efficacy of halofuginone and decoquinate in the treatment of cryptosporidiosis in veal calves. Lallemand, M., Villeneuve, A., Belda, J., Dubreuil, P. Vet. Rec. (2006) [Pubmed]
  10. Halofuginone inhibition of COL1A2 promoter activity via a c-Jun-dependent mechanism. McGaha, T.L., Kodera, T., Spiera, H., Stan, A.C., Pines, M., Bona, C.A. Arthritis Rheum. (2002) [Pubmed]
  11. Halofuginone, a collagen type I inhibitor improves liver regeneration in cirrhotic rats. Spira, G., Mawasi, N., Paizi, M., Anbinder, N., Genina, O., Alexiev, R., Pines, M. J. Hepatol. (2002) [Pubmed]
  12. Halofuginone inhibits NF-kappaB and p38 MAPK in activated T cells. Leiba, M., Cahalon, L., Shimoni, A., Lider, O., Zanin-Zhorov, A., Hecht, I., Sela, U., Vlodavsky, I., Nagler, A. J. Leukoc. Biol. (2006) [Pubmed]
  13. Inhibition of collagen synthesis, smooth muscle cell proliferation, and injury-induced intimal hyperplasia by halofuginone. Nagler, A., Miao, H.Q., Aingorn, H., Pines, M., Genina, O., Vlodavsky, I. Arterioscler. Thromb. Vasc. Biol. (1997) [Pubmed]
  14. Efficacy of halofuginone lactate against Cryptosporidium parvum in calves. Villacorta, I., Peeters, J.E., Vanopdenbosch, E., Ares-Mazás, E., Theys, H. Antimicrob. Agents Chemother. (1991) [Pubmed]
  15. Inhibition of glomerular mesangial cell proliferation and extracellular matrix deposition by halofuginone. Nagler, A., Katz, A., Aingorn, H., Miao, H.Q., Condiotti, R., Genina, O., Pines, M., Vlodavsky, I. Kidney Int. (1997) [Pubmed]
  16. Discriminant analysis of antibiotic resistance patterns in fecal streptococci, a method to differentiate human and animal sources of fecal pollution in natural waters. Wiggins, B.A. Appl. Environ. Microbiol. (1996) [Pubmed]
  17. Treatment with halofuginone results in marked growth inhibition of a von Hippel-Lindau pheochromocytoma in vivo. Gross, D.J., Reibstein, I., Weiss, L., Slavin, S., Dafni, H., Neeman, M., Pines, M., Nagler, A. Clin. Cancer Res. (2003) [Pubmed]
  18. Smad3 as a mediator of the fibrotic response. Flanders, K.C. International journal of experimental pathology. (2004) [Pubmed]
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