Heat shock proteins (HSPs) and chaperones are highly conserved stress-induced factors. They regulate not only
protein folding and stability but are also actively involved in protein transport and transcriptional regulation. HSPs have
cytoprotective roles and are essential for cancer cell survival. Noteworthy, HSPs are often upregulated in cancer. Therefore,
HSPs emerged as drug targets for cancer therapy. Especially for prostate cancer (PCa) therapy, a battery of different
compounds has been identified that act with different modes to inhibit PCa growth. The androgen receptor (AR) is a major
player in PCa progression and is a well-known interacting factor of HSPs. Since the AR function is very dependent on
HSP activity, many emerging compounds address the AR-associated HSPs as novel drug targets. Here, we provide an insight
into the different classes of HSPs, their association with the human AR, the role of HSPs in human PCa development
and review also the targeting of HSPs in human PCa. Further, the function and the underlying molecular mechanisms of
specific compounds that are currently under investigation for the use against PCa growth will be comprehensively summarized.
Keywords: Androgen receptor, chaperones, heat shock proteins, prostate cancer therapy.
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