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

Mofarotene     4-[2-[4-[(E)-2-(5,5,8,8- tetramethyl-6,7...

Synonyms: SureCN62905, CHEMBL146506, LS-2095, NSC-658402, NSC658402, ...
 
 
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Disease relevance of NSC658402

 

High impact information on NSC658402

  • The effect of the arotinoid mofarotene (Ro 40-8757; 4-[2-[p-[(E)- 2(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)- propenyl]phenoxy]ethyl]morpholine) on stromal cell-mediated hematopoiesis was examined in murine long-term bone marrow cultures [5].
  • However, after mofarotene treatment ceased, progenitor cell levels began increasing immediately, and cell production reached plateau levels comparable with those of control cultures within 4 weeks [5].
  • Mofarotene (Ro 40-8757) inhibits hematopoiesis in vitro by preventing maturation from primitive progenitor cells [5].
  • Mofarotene did not inhibit colony formation by bone marrow cells stimulated by exogenous growth factors and did not decrease production of growth factors by stromal cells in the cultures, as determined by functional assays and by mRNA levels [5].
  • In the search for retinoids active against Burkitt's lymphoma (BL), we found that the arotinoid mofarotene (Ro 40-8757) induced strong antiproliferative and apoptotic responses in most established BL cell lines as well as in primary BL cells [1].
 

Chemical compound and disease context of NSC658402

  • In conclusion, our data demonstrate that mofarotene, an already almost forgotten synthetic retinoid, shows interesting effects on melanoma cells, which may be relevant for a slowdown of tumour spread [4].
 

Biological context of NSC658402

 

Anatomical context of NSC658402

 

Associations of NSC658402 with other chemical compounds

  • The retinoids, all-trans and 9-cis retinoic acids, did not affect the expression of NDI in MDA-MB-231 cells, demonstrating that mofarotene was not acting through the nuclear retinoic-acid receptors [3].
 

Gene context of NSC658402

 

Analytical, diagnostic and therapeutic context of NSC658402

References

  1. Inhibition of oxidative phosphorylation underlies the antiproliferative and proapoptotic effects of mofarotene (Ro 40-8757) in Burkitt's lymphoma cells. Cariati, R., Zancai, P., Righetti, E., Rizzo, S., De Rossi, A., Boiocchi, M., Dolcetti, R. Oncogene (2003) [Pubmed]
  2. Arotinoid mofarotene (RO40-8757) up-regulates p21 and p27 during growth inhibition of pancreatic cancer cell lines. Kawa, S., Nikaido, T., Aoki, Y., Zhai, Y., Kumagaya, T., Furihata, K., Fujii, S., Kiyosawa, K. Int. J. Cancer (1997) [Pubmed]
  3. Down-regulation of mitochondrial gene expression by the anti-tumor arotinoid mofarotene (Ro 40-8757). Uchida, T., Inagaki, N., Furuichi, Y., Eliason, J.F. Int. J. Cancer (1994) [Pubmed]
  4. Mofarotene-induced inhibition of melanoma cell motility by increasing vinculin-containing focal contacts. Helige, C., Hofmann-Wellenhof, R., Fink-Puches, R., Smolle, J. Melanoma Res. (2004) [Pubmed]
  5. Mofarotene (Ro 40-8757) inhibits hematopoiesis in vitro by preventing maturation from primitive progenitor cells. Eliason, J.F., Baumgartner, M., Yoshikubo, T., Hirabayashi, Y., Mitsui, H., Inoue, T. Blood (1995) [Pubmed]
  6. Metabolism of mofarotene in hepatocytes and liver microsomes from different species. Comparison with in vivo data and evaluation of the cytochrome P450 isoenzymes involved in human biotransformation. Valles, B., Schiller, C.D., Coassolo, P., De Sousa, G., Wyss, R., Jaeck, D., Viger-Chougnet, A., Rahmani, R. Drug Metab. Dispos. (1995) [Pubmed]
  7. In vivo and in vitro kinetics of mofarotene in mouse, rat, dog and man. Vallès, B., Ba, B., Wyss, R., Reigner, B., Coassolo, P. European journal of drug metabolism and pharmacokinetics. (1995) [Pubmed]
 
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