17-AAG (also known as Tanespimycin) is a less toxic and more stable semi-synthetic derivative of Geldanamycin. It binds to Hsp90 (Heat Shock Protein 90) and is 100-fold higher affinity for Hsp90 derived from tumor cells compared to Hsp90 from normal cells. Hsp90 binds to client proteins, which are signaling proteins. The client proteins, which are induced to be degraded by 17-AAG, are key cancer relevant targets like mutated p53, Bcr-Abl, Her2, Akt, Raf-1, B-Raf and others.
For example, it is reported that Her2 is induced to be degraded in breast by 17-AAG. In addition, there is a study of spinal and bulbar muscular atrophy (SBMA) to explain that 17-AAG works to mutant Androgen receptor (AR) which is one of the client proteins of it. It also increases the activity of antitumor agents such as Taxol2, Cisplatin3 and UCN-014.
• Inhibitor of Hsp90 and its client proteins
• Anti-tumor agent
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|UN #'S||Not Applicable|