KU Leuven: KU Leuven researchers may find new treatment method for metastatic prostate cancer

Researchers from KU Leuven have discovered a promising new method for the treatment of metastatic prostate cancer. In that case, the male hormones in the patient are traditionally suppressed or inhibited with medication in order to slow down the disease. But after some time, the cancer cells become resistant to that medication. The new treatment method, on the other hand, also inhibits the action of the male hormone in resistant cells. The research appears today in the authoritative journal Molecular Cancer Therapeutics of the American Association for Cancer Research.

Prostate cancer, the most common cancer in men, is caused by cells that multiply uncontrollably in the tissue of the prostate. The prostate cancer cells can later spread in the body and form metastases. Hormone therapy is often used in this phase to slow the growth of the cancer. This therapy blocks the action of the male hormone testosterone.

However, the drugs currently used for this, androgen receptor inhibitors, only work temporarily, because the tumors become resistant. Discovering new ways to inhibit the action of the male hormone is therefore crucial.

A team around professors Arnout Voet and Frank Claessens (KU Leuven) have now discovered a completely new site on the androgen receptor (the protein to which testosterone binds) to which drugs can bind to suppress the action of the male hormone, and thus the inhibit cancer growth. The place was called the DIM pocket . Further research also identified molecules, active substances, that bind to the DIM pocket .

Because the molecules attach themselves to the DIM pocket , the androgen receptor can no longer bind to the DNA strand, and the genes that drive cancer development are switched off.

“We are very pleased that our basic research into the functioning of the androgen receptor is being translated into new possible treatments,” says Professor Frank Claessens.

We now have to make the molecules more powerful and ensure that there are no side effects for human use.

– professor Arnout Voet

“The discovery of this DIM pocket opens the way to completely new treatments and drugs that will act on the interaction between proteins such as the androgen receptor. Together with the molecules we identified, we have a proof of concept for such a treatment. The molecules do not only work on their own, but in combination with existing therapies they are even more efficient at suppressing the cancer cells. We now have to make the molecules more powerful and ensure that there are no side effects for human use,” adds Professor Arnout Voet.

The researchers are also hopeful that the DIM pocket can also be used in the treatment of other disorders in which similar receptors play a role. “What we are now going to investigate is whether molecules in the DIM pocket of other receptors can also bind molecules to treat other cancers and immune disorders,” said researcher Christine Helsen.