Mutations May Cause Prostate Cancer Patients to Become Resistant to BET Inhibitors, Study Says

Mutations May Cause Prostate Cancer Patients to Become Resistant to BET Inhibitors, Study Says
Mutations in the SPOP gene in prostate cancer are a reason patients often develop resistance to a class of treatment known as BET inhibitors, Mayo Clinic researchers report. This finding is in the study “Intrinsic BET inhibitor resistance in SPOP-mutated prostate cancer is mediated by BET protein stabilization and AKT–mTORC1 activation,” published in the journal Nature Medicine. BET proteins are expressed in most cells and play a role in activating the expression of cancer-promoting genes. Small-molecule inhibitors that target BET proteins have been developed and are currently in clinical trials as treatments for different types of cancer. But resistance to BET inhibitors has been widely reported in people with prostate cancer. SPOP is an enzyme that works to degrade certain proteins. Analysis of whole-genome and exome sequencing studies, which are conducted to spot mutations, found that SPOP is the most frequently mutated gene in patients with primary prostate cancer. Interestingly, the mutations tend to be in the active domain of the protein, which indicates that a loss of SPOP degradation may play a role in the disease. To further investigate the role of SPOP mutations in prostate cancer, researchers conducted experiments to determine the proteins that SPOP interacts with. While they discovered that SPOP interacts with many proteins, BET proteins were at the top of the list. The work al
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