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Chemical Compound Review

SL-1846     7-hydroxy-8-methoxy-7-[2- methyl-3-(3...

Synonyms: LS-99627, AC1L1I25, C16H24O5
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Disease relevance of Graphinone


High impact information on Graphinone


Biological context of Graphinone

  • Comparison of the Type I enzyme with the previously reported complex of ovalicin with Type II MetAP shows that the active site of the former is reduced in size and would incur steric clashes with the bound inhibitor [8].
  • Among the other three compounds, only ovalicin showed inhibitory activity (IC50, 27 microM) against MH60 cells [1].
  • QSAR of the inhibition of angiogenesis by TNP-470 and ovalicin analogues: another example of an allosteric interaction [9].

Anatomical context of Graphinone


Associations of Graphinone with other chemical compounds


Gene context of Graphinone

  • Here we report that S100A4 physically interacts with methionine aminopeptidase 2 (MetAP2), the primary target for potent angiogenesis inhibitors, fumagillin and ovalicin [13].
  • This Protac consisted of an SCF(beta-TRCP)-binding phosphopeptide derived from IkappaBalpha linked to ovalicin, which covalently binds MetAP-2 [14].

Analytical, diagnostic and therapeutic context of Graphinone


  1. Chlovalicin, a new cytocidal antibiotic produced by Sporothrix sp. FO-4649. I. Taxonomy, fermentation, isolation and biological activities. Hayashi, M., Kim, Y.P., Takamatsu, S., Preeprame, S., Komiya, T., Masuma, R., Tanaka, H., Komiyama, K., Omura, S. J. Antibiot. (1996) [Pubmed]
  2. Enhanced toxicity of the immunosuppressant ovalicin upon application to the skin. Stähelin, H. Experientia (1988) [Pubmed]
  3. Investigations into microsporidian methionine aminopeptidase type 2: a therapeutic target for microsporidiosis. Zhang, H., Huang, H., Cali, A., Takvorian, P.M., Feng, X., Zhou, G., Weiss, L.M. Folia Parasitol. (2005) [Pubmed]
  4. Protacs: chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradation. Sakamoto, K.M., Kim, K.B., Kumagai, A., Mercurio, F., Crews, C.M., Deshaies, R.J. Proc. Natl. Acad. Sci. U.S.A. (2001) [Pubmed]
  5. 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]
  6. A single amino acid residue defines the difference in ovalicin sensitivity between type I and II methionine aminopeptidases. Brdlik, C.M., Crews, C.M. J. Biol. Chem. (2004) [Pubmed]
  7. Letter: Application of carbon-13 magnetic resonance to isoprenoid biosynthesis. I. Ovalicin. Cane, D.E., Levin, R.H. J. Am. Chem. Soc. (1975) [Pubmed]
  8. Structural basis for the functional differences between type I and type II human methionine aminopeptidases. Addlagatta, A., Hu, X., Liu, J.O., Matthews, B.W. Biochemistry (2005) [Pubmed]
  9. QSAR of the inhibition of angiogenesis by TNP-470 and ovalicin analogues: another example of an allosteric interaction. Mekapati, S.B., Hansch, C. Bioorg. Med. Chem. (2001) [Pubmed]
  10. On the mode of action of the immunosuppressive sesquiterpene ovalicin. Zimmermann, W.A., Hartmann, G.R. Eur. J. Biochem. (1981) [Pubmed]
  11. Selective inhibition of amino-terminal methionine processing by TNP-470 and ovalicin in endothelial cells. Turk, B.E., Griffith, E.C., Wolf, S., Biemann, K., Chang, Y.H., Liu, J.O. Chem. Biol. (1999) [Pubmed]
  12. 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]
  13. Methionine aminopeptidase 2 is a new target for the metastasis-associated protein, S100A4. Endo, H., Takenaga, K., Kanno, T., Satoh, H., Mori, S. J. Biol. Chem. (2002) [Pubmed]
  14. Development of Protacs to target cancer-promoting proteins for ubiquitination and degradation. Sakamoto, K.M., Kim, K.B., Verma, R., Ransick, A., Stein, B., Crews, C.M., Deshaies, R.J. Mol. Cell Proteomics (2003) [Pubmed]
  15. Antimicrosporidial activities of fumagillin, TNP-470, ovalicin, and ovalicin derivatives in vitro and in vivo. Didier, P.J., Phillips, J.N., Kuebler, D.J., Nasr, M., Brindley, P.J., Stovall, M.E., Bowers, L.C., Didier, E.S. Antimicrob. Agents Chemother. (2006) [Pubmed]
  16. Synthetic analogues of TNP-470 and ovalicin reveal a common molecular basis for inhibition of angiogenesis and immunosuppression. Turk, B.E., Su, Z., Liu, J.O. Bioorg. Med. Chem. (1998) [Pubmed]
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