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Chemical Compound Review

trapoxin A     (3S,6S,9S,12R)-3,6-dibenzyl- 9-[6-[(2S)...

Synonyms: LS-172860, AC1L3TK4, C34H42N4O6, 133155-89-2
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Disease relevance of trapoxin


High impact information on trapoxin


Biological context of trapoxin


Anatomical context of trapoxin

  • Trapoxin (cyclo-(L-phenylalanyl-L-phenylalanyl-D-pipecolinyl-L-2-amino-8- oxo-9,10-epoxy-decanoyl)) is a fungal product that induces morphological reversion from transformed to normal in sis-transformed NIH3T3 fibroblasts [13].
  • Actin stress fiber could be detected after trapoxin treatment [14].

Gene context of trapoxin

  • This deacetylase activity is inhibited by trichostatin, trapoxin, and butyrate in vitro to the same degree as the deacetylase activity associated to HDAC1p [15].
  • Among other genes, the small GTPase RhoB was found to be significantly upregulated by TPX and repressed by HDAC1 [16].
  • Conversely, the overexpression of constitutively active mutants of H-ras or MEK1 proteins had little or no effect on ChAT promoter activity, but strongly synergized with trapoxin [4].
  • The overexpression of dominant negative mutants of H-ras or ERK2 proteins depressed ChAT promoter activation by trapoxin in transient transfection assays [4].
  • We now show that trapoxin and butyrate triggered a rapid and transient phosphorylation of ERK1/2 kinases, that was suppressed by PD98059, a highly specific inhibitor of MAP kinase kinase MEK1 [4].

Analytical, diagnostic and therapeutic context of trapoxin


  1. Transcriptional activation and chromatin remodeling of the HIV-1 promoter in response to histone acetylation. Van Lint, C., Emiliani, S., Ott, M., Verdin, E. EMBO J. (1996) [Pubmed]
  2. Rapid induction of histone hyperacetylation and cellular differentiation in human breast tumor cell lines following degradation of histone deacetylase-1. Zhou, Q., Melkoumian, Z.K., Lucktong, A., Moniwa, M., Davie, J.R., Strobl, J.S. J. Biol. Chem. (2000) [Pubmed]
  3. Inhibition of histone deacetylases induces bovine leukemia virus expression in vitro and in vivo. Merezak, C., Reichert, M., Van Lint, C., Kerkhofs, P., Portetelle, D., Willems, L., Kettmann, R. J. Virol. (2002) [Pubmed]
  4. Activation of the MAP kinase cascade by histone deacetylase inhibitors is required for the stimulation of choline acetyltransferase gene promoter. Espinos, E., Weber, M.J. Brain Res. Mol. Brain Res. (1998) [Pubmed]
  5. Histone deacetylase activity is required for full transcriptional repression by mSin3A. Hassig, C.A., Fleischer, T.C., Billin, A.N., Schreiber, S.L., Ayer, D.E. Cell (1997) [Pubmed]
  6. A mammalian histone deacetylase related to the yeast transcriptional regulator Rpd3p. Taunton, J., Hassig, C.A., Schreiber, S.L. Science (1996) [Pubmed]
  7. Potent histone deacetylase inhibitors built from trichostatin A and cyclic tetrapeptide antibiotics including trapoxin. Furumai, R., Komatsu, Y., Nishino, N., Khochbin, S., Yoshida, M., Horinouchi, S. Proc. Natl. Acad. Sci. U.S.A. (2001) [Pubmed]
  8. Depudecin induces morphological reversion of transformed fibroblasts via the inhibition of histone deacetylase. Kwon, H.J., Owa, T., Hassig, C.A., Shimada, J., Schreiber, S.L. Proc. Natl. Acad. Sci. U.S.A. (1998) [Pubmed]
  9. A role for histone deacetylase activity in HDAC1-mediated transcriptional repression. Hassig, C.A., Tong, J.K., Fleischer, T.C., Owa, T., Grable, P.G., Ayer, D.E., Schreiber, S.L. Proc. Natl. Acad. Sci. U.S.A. (1998) [Pubmed]
  10. Induction of gamma-globin by histone deacetylase inhibitors. McCaffrey, P.G., Newsome, D.A., Fibach, E., Yoshida, M., Su, M.S. Blood (1997) [Pubmed]
  11. Trichostatin A and trapoxin: novel chemical probes for the role of histone acetylation in chromatin structure and function. Yoshida, M., Horinouchi, S., Beppu, T. Bioessays (1995) [Pubmed]
  12. Temporally restricted spatial localization of acetylated isoforms of histone H4 and RNA polymerase II in the 2-cell mouse embryo. Worrad, D.M., Turner, B.M., Schultz, R.M. Development (1995) [Pubmed]
  13. Trapoxin, an antitumor cyclic tetrapeptide, is an irreversible inhibitor of mammalian histone deacetylase. Kijima, M., Yoshida, M., Sugita, K., Horinouchi, S., Beppu, T. J. Biol. Chem. (1993) [Pubmed]
  14. A novel tetracyclic peptide, trapoxin, induces phenotypic change from transformed to normal in sis-oncogene-transformed NIH3T3 cells. Yoshida, H., Sugita, K. Jpn. J. Cancer Res. (1992) [Pubmed]
  15. Characterization of a human RPD3 ortholog, HDAC3. Emiliani, S., Fischle, W., Van Lint, C., Al-Abed, Y., Verdin, E. Proc. Natl. Acad. Sci. U.S.A. (1998) [Pubmed]
  16. Histone deacetylase 1 represses the small GTPase RhoB expression in human nonsmall lung carcinoma cell line. Wang, S., Yan-Neale, Y., Fischer, D., Zeremski, M., Cai, R., Zhu, J., Asselbergs, F., Hampton, G., Cohen, D. Oncogene (2003) [Pubmed]
  17. Histone deacetylase inhibition selectively alters the activity and expression of cell cycle proteins leading to specific chromatin acetylation and antiproliferative effects. Sambucetti, L.C., Fischer, D.D., Zabludoff, S., Kwon, P.O., Chamberlin, H., Trogani, N., Xu, H., Cohen, D. J. Biol. Chem. (1999) [Pubmed]
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