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Retaspimycin is a water-soluble hydroquinone hydrochloride salt inhibitor of Hsp90 [1].

Hsp90 is a member of the Hsp family. The other members of this protein family are Hsp40, Hsp70 and so on. These proteins act as molecule chaperons and participate in many cellular processes. When cells are exposed in stress, some proteins become unstable, accumulate to form aggregates and subsequently cause cell apoptosis. In this situation, Hsps will help their client proteins folding correctly, accompany them to be translocated to the correct location and thus prevent the cells from apoptosis. Hsps are required for cancer cells development. They are found to overexpress in a variety of cancer cells. Therefore, the inhibitors of Hsp are thought to be attractive therapy for cancer treatment. As an inhibitor of Hsp90, retaspimycin works through binding to the ATP-binding pocket of Hsp90 N-terminal [1].

In both RPMI-8826 and MM1.S cells, treatment of retaspimycin resulted in degradation of the Hsp90 client proteins, for instance, c-RAF and Her2. It also caused increased levels of Hsp70. Besides that, retaspimycin is found to prevent RPMI-8826 cells from secreting the immunoglobulin light chain. In breast cancer cells which are resistant to trastuzumab, treatment of retaspimycin potently caused Her2 degradation and resulted in tumor growth suppression and cell apoptosis [1].

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