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Chemical Compound Review

Fugillin     (2Z,4E,6E,8E)-10-[[5-methoxy- 4-[2-methyl-3...

Synonyms: Fugilin, Fumidil, Amebacilin, fumagillin, Amebacillin, ...
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Disease relevance of Fumidil


High impact information on Fumidil


Chemical compound and disease context of Fumidil


Biological context of Fumidil

  • A 1.8 A resolution crystal structure of free and inhibited human MetAP-2 shows a covalent bond formed between a reactive epoxide of fumagillin and histidine-231 in the active site of MetAP-2 [6].
  • Inhibition of hepatic stellate cell proliferation and activation by the semisynthetic analogue of fumagillin TNP-470 in rats [12].
  • In this study, we investigated, by microarray analysis, the effects of two known antiangiogenic agents (endostatin and fumagillin) on the gene expression profiles of human umbilical vein endothelial cells (HUVEC) in order to elucidate pathways common to the effects of these agents [13].
  • Consistently, fumagillin induced apoptosis, owing to early mitochondrial damage, in malignant, but not in normal mesothelial cells [14].
  • Fumagillin, an antibiotic reported to exhibit selective activity against ras transformed cells showed very marked and selective cytostatic effects against HT1080scc2 cells with IC50 values as low as 1 x 10(-11) M [15].

Anatomical context of Fumidil


Associations of Fumidil with other chemical compounds


Gene context of Fumidil

  • In the MAP1A KO context, modulating MAP2 activity by treatment with various concentrations of the specific drug fumagillin impaired plant development, with particularly strong effects on the root system [26].
  • Bone morphogenetic protein (BMP) is a potent inducer of ectopic bone formation, and TNP-470, a synthetic analog of fumagillin, is an antiangiogenic agent that strongly inhibits neovascular formation in vivo [27].
  • When HUVEC and A549 cells were treated simultaneously with MetAP-2 siRNA and PPI-2458, or fumagillin, which irreversibly inhibit MetAP-2 enzyme activity, no additive effect on maximum growth inhibition was observed [28].
  • We show that fumagillin increases the stability of p67 by decreasing its turnover rate [18].
  • The binding is highly specific as judged by the failure of fumagillin to inhibit MetAP-1 in vivo [7].

Analytical, diagnostic and therapeutic context of Fumidil


  1. Synthetic analogues of fumagillin that inhibit angiogenesis and suppress tumour growth. Ingber, D., Fujita, T., Kishimoto, S., Sudo, K., Kanamaru, T., Brem, H., Folkman, J. Nature (1990) [Pubmed]
  2. The anti-angiogenic agent fumagillin covalently modifies a conserved active-site histidine in the Escherichia coli methionine aminopeptidase. Lowther, W.T., McMillen, D.A., Orville, A.M., Matthews, B.W. Proc. Natl. Acad. Sci. U.S.A. (1998) [Pubmed]
  3. Inhibition of tumor growth and metastasis of rodent tumors by the angiogenesis inhibitor O-(chloroacetyl-carbamoyl)fumagillol (TNP-470; AGM-1470). Yamaoka, M., Yamamoto, T., Masaki, T., Ikeyama, S., Sudo, K., Fujita, T. Cancer Res. (1993) [Pubmed]
  4. Suppression of hepatoma growth and angiogenesis by a fumagillin derivative TNP470: possible involvement of nitric oxide synthase. Yoshida, T., Kaneko, Y., Tsukamoto, A., Han, K., Ichinose, M., Kimura, S. Cancer Res. (1998) [Pubmed]
  5. Fumagillin analog in the treatment of Kaposi's sarcoma: a phase I AIDS Clinical Trial Group study. AIDS Clinical Trial Group No. 215 Team. Dezube, B.J., Von Roenn, J.H., Holden-Wiltse, J., Cheung, T.W., Remick, S.C., Cooley, T.P., Moore, J., Sommadossi, J.P., Shriver, S.L., Suckow, C.W., Gill, P.S. J. Clin. Oncol. (1998) [Pubmed]
  6. Structure of human methionine aminopeptidase-2 complexed with fumagillin. Liu, S., Widom, J., Kemp, C.W., Crews, C.M., Clardy, J. Science (1998) [Pubmed]
  7. The anti-angiogenic agent fumagillin covalently binds and inhibits the methionine aminopeptidase, MetAP-2. Sin, N., Meng, L., Wang, M.Q., Wen, J.J., Bornmann, W.G., Crews, C.M. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  8. A fumagillin derivative angiogenesis inhibitor, AGM-1470, inhibits activation of cyclin-dependent kinases and phosphorylation of retinoblastoma gene product but not protein tyrosyl phosphorylation or protooncogene expression in vascular endothelial cells. Abe, J., Zhou, W., Takuwa, N., Taguchi, J., Kurokawa, K., Kumada, M., Takuwa, Y. Cancer Res. (1994) [Pubmed]
  9. System for Expression of Microsporidian Methionine Amino Peptidase Type 2 (MetAP2) in the Yeast Saccharomyces cerevisiae. Upadhya, R., Zhang, H.S., Weiss, L.M. Antimicrob. Agents Chemother. (2006) [Pubmed]
  10. Microsporidial keratoconjunctivitis in a healthy contact lens wearer without human immunodeficiency virus infection. Theng, J., Chan, C., Ling, M.L., Tan, D. Ophthalmology (2001) [Pubmed]
  11. Effect of angiogenesis inhibitor TNP-470 on vascular formation in pituitary tumors induced by estrogen in rats. Takechi, A. Neurol. Med. Chir. (Tokyo) (1994) [Pubmed]
  12. Inhibition of hepatic stellate cell proliferation and activation by the semisynthetic analogue of fumagillin TNP-470 in rats. Wang, Y.Q., Ikeda, K., Ikebe, T., Hirakawa, K., Sowa, M., Nakatani, K., Kawada, N., Kaneda, K. Hepatology (2000) [Pubmed]
  13. Early genetic mechanisms underlying the inhibitory effects of endostatin and fumagillin on human endothelial cells. Mazzanti, C.M., Tandle, A., Lorang, D., Costouros, N., Roberts, D., Bevilacqua, G., Libutti, S.K. Genome Res. (2004) [Pubmed]
  14. Methionine aminopeptidase-2 regulates human mesothelioma cell survival: role of Bcl-2 expression and telomerase activity. Catalano, A., Romano, M., Robuffo, I., Strizzi, L., Procopio, A. Am. J. Pathol. (2001) [Pubmed]
  15. A novel cell-based assay for the evaluation of anti-ras compounds. Jenkins, D.C., Stables, J.N., Wilkinson, J., Topley, P., Holmes, L.S., Linstead, D.J., Rapson, E.B. Br. J. Cancer (1993) [Pubmed]
  16. The fumagillin analogue TNP-470 inhibits DNA synthesis of vascular smooth muscle cells stimulated by platelet-derived growth factor and insulin-like growth factor-I. Possible involvement of cyclin-dependent kinase 2. Koyama, H., Nishizawa, Y., Hosoi, M., Fukumoto, S., Kogawa, K., Shioi, A., Morii, H. Circ. Res. (1996) [Pubmed]
  17. Cerebrospinal fluid proteomic analysis reveals dysregulation of methionine aminopeptidase-2 expression in human and mouse neurofibromatosis 1-associated glioma. Dasgupta, B., Yi, Y., Hegedus, B., Weber, J.D., Gutmann, D.H. Cancer Res. (2005) [Pubmed]
  18. Treatment of cells with the angiogenic inhibitor fumagillin results in increased stability of eukaryotic initiation factor 2-associated glycoprotein, p67, and reduced phosphorylation of extracellular signal-regulated kinases. Datta, B., Majumdar, A., Datta, R., Balusu, R. Biochemistry (2004) [Pubmed]
  19. Angiogenesis inhibitor TNP-470 inhibits growth and metastasis of a hormone-independent rat prostatic carcinoma cell line. Miki, T., Nonomura, N., Nozawa, M., Harada, Y., Nishimura, K., Kojima, Y., Takahara, S., Okuyama, A. J. Urol. (1998) [Pubmed]
  20. Fumagillin suppresses HIV-1 infection of macrophages through the inhibition of Vpr activity. Watanabe, N., Nishihara, Y., Yamaguchi, T., Koito, A., Miyoshi, H., Kakeya, H., Osada, H. FEBS Lett. (2006) [Pubmed]
  21. Molecular recognition of angiogenesis inhibitors fumagillin and ovalicin by methionine aminopeptidase 2. Griffith, E.C., Su, Z., Niwayama, S., Ramsay, C.A., Chang, Y.H., Liu, J.O. Proc. Natl. Acad. Sci. U.S.A. (1998) [Pubmed]
  22. Targeted gene disruption of methionine aminopeptidase 2 results in an embryonic gastrulation defect and endothelial cell growth arrest. Yeh, J.R., Ju, R., Brdlik, C.M., Zhang, W., Zhang, Y., Matyskiela, M.E., Shotwell, J.D., Crews, C.M. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  23. Methionine aminopeptidase (type 2) is the common target for angiogenesis inhibitors AGM-1470 and ovalicin. Griffith, E.C., Su, Z., Turk, B.E., Chen, S., Chang, Y.H., Wu, Z., Biemann, K., Liu, J.O. Chem. Biol. (1997) [Pubmed]
  24. Susceptibility of Encephalitozoon cuniculi to several drugs in vitro. Franssen, F.F., Lumeij, J.T., van Knapen, F. Antimicrob. Agents Chemother. (1995) [Pubmed]
  25. Purification and characterization of factors produced by Aspergillus fumigatus which affect human ciliated respiratory epithelium. Amitani, R., Taylor, G., Elezis, E.N., Llewellyn-Jones, C., Mitchell, J., Kuze, F., Cole, P.J., Wilson, R. Infect. Immun. (1995) [Pubmed]
  26. Functional and developmental impact of cytosolic protein N-terminal methionine excision in Arabidopsis. Ross, S., Giglione, C., Pierre, M., Espagne, C., Meinnel, T. Plant Physiol. (2005) [Pubmed]
  27. Antiangiogenic agent (TNP-470) inhibition of ectopic bone formation induced by bone morphogenetic protein-2. Mori, S., Yoshikawa, H., Hashimoto, J., Ueda, T., Funai, H., Kato, M., Takaoka, K. Bone (1998) [Pubmed]
  28. Methionine aminopeptidases type I and type II are essential to control cell proliferation. Bernier, S.G., Taghizadeh, N., Thompson, C.D., Westlin, W.F., Hannig, G. J. Cell. Biochem. (2005) [Pubmed]
  29. Potential efficacy of fumagillin in intestinal microsporidiosis due to Enterocytozoon bieneusi in patients with HIV infection: results of a drug screening study. The French Microsporidiosis Study Group. Molina, J.M., Goguel, J., Sarfati, C., Chastang, C., Desportes-Livage, I., Michiels, J.F., Maslo, C., Katlama, C., Cotte, L., Leport, C., Raffi, F., Derouin, F., Modaï, J. AIDS (1997) [Pubmed]
  30. Diffusible component from the spore surface of the fungus Aspergillus fumigatus which inhibits the macrophage oxidative burst is distinct from gliotoxin and other hyphal toxins. Mitchell, C.G., Slight, J., Donaldson, K. Thorax (1997) [Pubmed]
  31. Interaction between tacrolimus and fumagillin in two kidney transplant recipients. Arzouk, N., Michelon, H., Snanoudj, R., Taburet, A.M., Durrbach, A., Furlan, V. Transplantation (2006) [Pubmed]
  32. TNP-470, an angiogenesis inhibitor, attenuates the development of allograft vasculopathy. Denton, M.D., Magee, C., Melter, M., Dharnidharka, V.R., Sayegh, M.H., Briscoe, D.M. Transplantation (2004) [Pubmed]
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