Completed Cancer Digestion, Kidneys & Other Organs

Novel drug candidates for the treatment of castrate resistant prostate cancer

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Prostate cancer cells learn to grow without the male hormones that drugs are designed to cut off, and a company called CellCentric has identified an enzyme that drives this lethal adaptation. This matters because castration-resistant prostate cancer (CRPC) develops in 10–20% of prostate cancer patients and is the form of the disease that kills. Current treatments eventually fail because the cancer finds a way around hormone deprivation. CellCentric already has prototype compounds that block the newly identified enzyme, but these are not yet potent or stable enough to test in animals. If the team can optimise these inhibitors into drug-like molecules, they will test them in laboratory models of CRPC. Success would produce a candidate compound ready for human clinical trials—a potential new treatment for a form of prostate cancer that currently has limited options once hormone therapy stops working. This is early-stage drug discovery, not a cure in hand, but it targets a specific molecular mechanism that could give patients a new line of defence.

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Prostate cancer is the second leading cause of mortality among men. Initial treatments focus on reducing the levels of circulating male hormones in the body which the cancer requires for growth. Overtime however, in 10-20% of cases, the cancer cells circumvent this treatment and develop into ‘castration-resistant’ prostate cancer (CRPC). This is the lethal form of the disease. CellCentric have identified an enzyme that regulates the cellular processes that lead to the development of this lethal form of the disease. It is proposed to identify and optimise an inhibitor of this enzyme as a potential new drug for the treatment of CRPC. On-going research at CellCentric has identified prototype inhibitors of the enzyme. The research proposal aims to optimise these inhibitors so that they can be assessed for anti-tumour activity in models of CRPC. If these ‘proof of concept’ studies are successful, a candidate compound will be nominated for further evaluation in human clinical trials.

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Related Research

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Characterisation of a novel series of small molecule androgen receptor modulators in prostate cancer
Identifying New Drugs for the Treatment of Castrate Resistant Prostate Cancer: Targeting the Achilles' Heel of the Androgen Receptor.
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