An international team of researchers led by IRB Barcelona has discovered a new way to block some key proteins in prostate cancer. These are oncoproteins that belong to the group of so-called “transcription factors”, for which it has not yet been possible to design drugs to block or amplify their effect.
Specifically, the team discovered how it works to block the function of the androgen receptor, an essential transcription factor in this type of cancer, based on its tendency to form condensates. The logic followed can be used to optimize this transcription factor inhibitor for other oncoproteins.
Transcription factors are regulatory proteins that bind to DNA, turn genes on or off, and control the rate of transcription of DNA into messenger RNA, which is essential for protein synthesis. The team of researchers says that because of its central role in controlling the formation of new proteins, many diseases can be attributed to dysregulated transcription factors.
That’s why the group believes that inhibiting its activity, especially in cancer, offers “therapeutic potential.” But the difficulty is that the activation domains are “intrinsically disordered,” that is, they do not have a clear three-dimensional structure, and this makes it “virtually impossible” to design drugs that bind to the activation domains. .
In this context, the team led by Javier Salvatella, ICREA Research Professor, and Antoni Riera, Professor at the University of Barcelona, focused on the tendency of these intrinsically disordered proteins to form molecular condensates, and discovered that the mechanisms involved in condensation could be used to inhibit androgen receptor activity in prostate cancer.
“The logic we followed to optimize the androgen receptor inhibitor can be exploited to inhibit other transcription factors, opening new possibilities to address unmet medical needs,” said Salvatella, head of the Molecular Biophysics Laboratory at IRB Barcelona.
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