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Geldanamycin



Geldanamycin
Molecular formula C29H40N2O9
Identifiers
CAS number 30562-34-6
Properties
Molar mass 560.64 g/mol
Appearance Gold-yellow fine crystalline powder
Except where noted otherwise, data are given for
materials in their standard state
(at 25 °C, 100 kPa)

Infobox disclaimer and references

Geldanamycin is a benzoquinone ansamycin antibiotic that binds to Hsp90 (Heat Shock Protein 90) and alters its function. HSP90 client proteins play important roles in the regulation of the cell cycle, cell growth, cell survival, apoptosis, angiogenesis and oncogenesis.

Geldanamycin induces the degradation of proteins that are mutated in tumor cells such as v-Src, Bcr-Abl and p53 preferentially over their normal cellular counterparts. This effect is mediated via HSP90. Despite its potent antitumor potential, geldanamycin presents several major drawbacks as a drug candidate (namely, hepatotoxicity) that have led to the development of geldanamycin analogues, in particular analogues containing a derivatisation at the 17 position:

  • 17-AAG
  • 17-DMAG

References

  • Bedin M, Gaben AM, Saucier C, Mester J. Int J Cancer. 2004 May 1;109(5):643-52. Geldanamycin, an inhibitor of the chaperone activity of HSP90, induces MAPK-independent cell cycle arrest.
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Geldanamycin". A list of authors is available in Wikipedia.
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