erbB-2 oncogene inhibition by geldanamycin derivatives: synthesis, mechanism of action, and structure-activity relationships.

@article{Schnur1995erbB2OI,
  title={erbB-2 oncogene inhibition by geldanamycin derivatives: synthesis, mechanism of action, and structure-activity relationships.},
  author={Rodney Caughren Schnur and Marvin L. Corman and Randall James Gallaschun and Beth Anne Cooper and Michael F. Dee and J L Doty and M L Muzzi and Caroline Diorio and Elsa G. Barbacci and Penelope E Miller},
  journal={Journal of medicinal chemistry},
  year={1995},
  volume={38 19},
  pages={
          3813-20
        }
}
Overexpression of the erbB-2 oncogene has been linked to poor prognosis in breast, ovarian, and gastric cancers. Naturally occurring benzoquinoid ansamycin antibiotics herbimycin A, geldanamycin (GDM), and dihydrogeldanamycin were found to potently deplete p185, the erbB-2 oncoprotein, in human breast cancer SKBR-3 cells in culture. Chemistry efforts to modify selectively the ansa ring of GDM afforded derivatives with greater potency in vitro and in vivo. Analogs demonstrated inhibition of p185… CONTINUE READING

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