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Chemical Compound Review

Blenoxane     3-[[2-[2-[2-[[(2S,3R)-2- [[(2S,3S,4R)-4...

Synonyms: Bleocin, Bleomicin, bleomycin, Bleomicina, Bleomycins, ...
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Disease relevance of Bleomycins


Psychiatry related information on Bleomycins


High impact information on Bleomycins


Chemical compound and disease context of Bleomycins


Biological context of Bleomycins


Anatomical context of Bleomycins

  • The peak TGF-beta levels preceded the maximum collagen and noncollagen protein synthesis measured by [3H]proline incorporation into lung fibroblast explants of bleomycin-treated rats [22].
  • The effects of bleomycin were associated with translocation of p53 from the cytosol to the nucleus only in alveolar macrophages that had been exposed to the drug in vivo, suggesting that the lung microenvironment regulated p53 activation [19].
  • A specific role for NO was demonstrated in experiments with inducible nitric oxide synthase (iNOS)(-/)- macrophages, which failed to demonstrate nuclear p53 localization after in vivo bleomycin exposure [19].
  • These results indicate that in response to bleomycin, the T lymphocytes induce, by an undefined mechanism, an increase of the pulmonary TNF production, which leads to alveolar damage, growth of fibroblast, and collagen deposition [16].
  • We have shown that transgenic mice expressing Streptoalloteichus hindustanus (Sh) ble bleomycin resistance protein in pulmonary epithelial cells in the lungs are protected against bleomycin-induced toxicity in lungs [23].

Associations of Bleomycins with other chemical compounds


Gene context of Bleomycins

  • Transient gene transfer and expression of Smad7 prevents bleomycin-induced lung fibrosis in mice [28].
  • In addition, we found that expression of Smad7 transgene blocked Smad2 phosphorylation induced by bleomycin in mouse lungs [28].
  • Treatment of bleomycin-exposed animals with specific neutralizing anti-CXCL12 Ab's inhibited intrapulmonary recruitment of CD45(+)Col I(+)CXCR4(+) circulating fibrocytes and attenuated lung fibrosis [29].
  • In this study, we show that BLM function is specifically required to properly relocalize the RAD50/MRE11/NBS1 (RMN) complex at sites of replication arrest, but is not essential in the activation of BRCA1 either after stalled replication forks or gamma-rays [30].
  • A large decrease in mosaic clone frequency is observed when Rrp1 overexpression precedes treatment with gamma-rays, bleomycin, or paraquat [31].

Analytical, diagnostic and therapeutic context of Bleomycins


  1. Bleomycin for hypercalcemia due to cancer. Nijjar, T., Brandes, L.J. N. Engl. J. Med. (1983) [Pubmed]
  2. Bleomycin-resistant DNA synthesis in ataxia telangiectasia cells. Cramer, P., Painter, R.B. Nature (1981) [Pubmed]
  3. Reversibility of severe bleomycin-induced pneumonitis. Brown, W.G., Hasan, F.M., Barbee, R.A. JAMA (1978) [Pubmed]
  4. Young adults with head and neck cancer express increased susceptibility to mutagen-induced chromosome damage. Schantz, S.P., Hsu, T.C., Ainslie, N., Moser, R.P. JAMA (1989) [Pubmed]
  5. Alterations in pulmonary protective enzymes following systemic bleomycin treatment in mice. Filderman, A.E., Genovese, L.A., Lazo, J.S. Biochem. Pharmacol. (1988) [Pubmed]
  6. Conformational flexibility of bleomycin-A2: a carbon-13 spin-lattice relaxation time study. Krishna, N.R., Dallas, J.L., Mooberry, E.S., Sakai, T.T., Allen, R.C., Levy, G.C., Glickson, J.D. Biochem. Biophys. Res. Commun. (1978) [Pubmed]
  7. Responses of Huntington's disease and ataxia telangiectasia lymphoblastoid cells to bleomycin. Imray, F.P., Kidson, C. Chem. Biol. Interact. (1983) [Pubmed]
  8. Toxic effects of bleomycin on the hypothalamus following its administration into a cystic craniopharyngioma. Haisa, T., Ueki, K., Yoshida, S. British journal of neurosurgery. (1994) [Pubmed]
  9. Therapy of advanced esophageal cancer with bleomycin, irradiation and combination of bleomycin with irradiation. Kolarić, K., Maricić, Z., Dujmović, I., Roth, A. Tumori. (1976) [Pubmed]
  10. A pivotal role of cytosolic phospholipase A(2) in bleomycin-induced pulmonary fibrosis. Nagase, T., Uozumi, N., Ishii, S., Kita, Y., Yamamoto, H., Ohga, E., Ouchi, Y., Shimizu, T. Nat. Med. (2002) [Pubmed]
  11. Bleomycin causes release of nucleosomes from chromatin and chromosomes. Kuo, M.T., Hsu, T.C. Nature (1978) [Pubmed]
  12. Crystal structure of a conserved protease that binds DNA: the bleomycin hydrolase, Gal6. Joshua-Tor, L., Xu, H.E., Johnston, S.A., Rees, D.C. Science (1995) [Pubmed]
  13. Potentiation of bleomycin lethality by anticalmodulin drugs: a role for calmodulin in DNA repair. Chafouleas, J.G., Bolton, W.E., Means, A.R. Science (1984) [Pubmed]
  14. Fatal pulmonary reaction from low doses of bleomycin. An idiosyncratic tissue response. Iacovino, J.R., Leitner, J., Abbas, A.K., Lokich, J.J., Snider, G.L. JAMA (1976) [Pubmed]
  15. Caveolin-1: a critical regulator of lung fibrosis in idiopathic pulmonary fibrosis. Wang, X.M., Zhang, Y., Kim, H.P., Zhou, Z., Feghali-Bostwick, C.A., Liu, F., Ifedigbo, E., Xu, X., Oury, T.D., Kaminski, N., Choi, A.M. J. Exp. Med. (2006) [Pubmed]
  16. Tumor necrosis factor/cachectin plays a key role in bleomycin-induced pneumopathy and fibrosis. Piguet, P.F., Collart, M.A., Grau, G.E., Kapanci, Y., Vassalli, P. J. Exp. Med. (1989) [Pubmed]
  17. Antitumor and toxic effects of combination chemotherapy with bleomycin and a phenothiazine anticalmodulin agent. Hait, W.N., Lazo, J.S., Chen, D.L., Gallichio, V.S., Filderman, A.E. J. Natl. Cancer Inst. (1988) [Pubmed]
  18. TGF-beta is a critical mediator of acute lung injury. Pittet, J.F., Griffiths, M.J., Geiser, T., Kaminski, N., Dalton, S.L., Huang, X., Brown, L.A., Gotwals, P.J., Koteliansky, V.E., Matthay, M.A., Sheppard, D. J. Clin. Invest. (2001) [Pubmed]
  19. Nitric oxide-dependent activation of p53 suppresses bleomycin-induced apoptosis in the lung. Davis, D.W., Weidner, D.A., Holian, A., McConkey, D.J. J. Exp. Med. (2000) [Pubmed]
  20. Inherited susceptibility to bleomycin-induced chromatid breaks in cultured peripheral blood lymphocytes. Cloos, J., Nieuwenhuis, E.J., Boomsma, D.I., Kuik, D.J., van der Sterre, M.L., Arwert, F., Snow, G.B., Braakhuis, B.J. J. Natl. Cancer Inst. (1999) [Pubmed]
  21. Changes in procoagulant and fibrinolytic gene expression during bleomycin-induced lung injury in the mouse. Olman, M.A., Mackman, N., Gladson, C.L., Moser, K.M., Loskutoff, D.J. J. Clin. Invest. (1995) [Pubmed]
  22. Macrophage production of transforming growth factor beta and fibroblast collagen synthesis in chronic pulmonary inflammation. Khalil, N., Bereznay, O., Sporn, M., Greenberg, A.H. J. Exp. Med. (1989) [Pubmed]
  23. Prevention of bleomycin-induced pulmonary fibrosis after adenovirus-mediated transfer of the bacterial bleomycin resistance gene. Tran, P.L., Weinbach, J., Opolon, P., Linares-Cruz, G., Reynes, J.P., Grégoire, A., Kremer, E., Durand, H., Perricaudet, M. J. Clin. Invest. (1997) [Pubmed]
  24. Nitric oxide upregulates expression of DNA-PKcs to protect cells from DNA-damaging anti-tumour agents. Xu, W., Liu, L., Smith, G.C., Charles, G. Nat. Cell Biol. (2000) [Pubmed]
  25. Hypersensitivity of cultured ataxia-telangiectasia cells to etoposide. Henner, W.D., Blazka, M.E. J. Natl. Cancer Inst. (1986) [Pubmed]
  26. Effect of heating on lethality due to hyperthermia and selected chemotherapeutic drugs. Herman, T.S., Sweets, C.C., White, D.M., Gerner, E.W. J. Natl. Cancer Inst. (1982) [Pubmed]
  27. Effects of nicotinamide, isonicotinamide, and bleomycin on DNA synthesis and repair in rat hepatocytes and hepatoma cells. Barra, R., Randolph, V., Sumas, M., Lanighan, K., Lea, M.A. J. Natl. Cancer Inst. (1982) [Pubmed]
  28. Transient gene transfer and expression of Smad7 prevents bleomycin-induced lung fibrosis in mice. Nakao, A., Fujii, M., Matsumura, R., Kumano, K., Saito, Y., Miyazono, K., Iwamoto, I. J. Clin. Invest. (1999) [Pubmed]
  29. Circulating fibrocytes traffic to the lungs in response to CXCL12 and mediate fibrosis. Phillips, R.J., Burdick, M.D., Hong, K., Lutz, M.A., Murray, L.A., Xue, Y.Y., Belperio, J.A., Keane, M.P., Strieter, R.M. J. Clin. Invest. (2004) [Pubmed]
  30. Bloom's syndrome protein is required for correct relocalization of RAD50/MRE11/NBS1 complex after replication fork arrest. Franchitto, A., Pichierri, P. J. Cell Biol. (2002) [Pubmed]
  31. Overexpression of a Rrp1 transgene reduces the somatic mutation and recombination frequency induced by oxidative DNA damage in Drosophila melanogaster. Szakmary, A., Huang, S.M., Chang, D.T., Beachy, P.A., Sander, M. Proc. Natl. Acad. Sci. U.S.A. (1996) [Pubmed]
  32. Craniopharyngiomas. Karavitaki, N., Cudlip, S., Adams, C.B., Wass, J.A. Endocr. Rev. (2006) [Pubmed]
  33. Large-dose bleomycin therapy and pulmonary toxicity. A possible role of prior radiotherapy. Samuels, M.L., Johnson, D.E., Holoye, P.Y., Lanzotti, V.J. JAMA (1976) [Pubmed]
  34. Routine pulmonary function tests during bleomycin therapy. Tests may be ineffective and potentially misleading. Lewis, B.M., Izbicki, R. JAMA (1980) [Pubmed]
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