Imma Perfetto
Cosmos science journalist
A team at Monash University in Victoria developing a hormone-free, reversible male contraceptive has now figured out the 3D structure of one of their primary therapeutic targets – the P2X1-purinergic receptor (P2X1).
According to Dr Sab Ventura from the Monash Institute of Pharmaceutical Sciences (MIPS), this has been the main stumbling block that has so far hindered the team from progressing the drug discovery program to the next stage.
“Our primary goal is to develop a male contraceptive pill that is not only hormone-free but also bypasses side effects such as long-term irreversible impacts on fertility, making it suitable for young men seeking contraceptive options,” says Ventura.
In previous research in mice, the team showed that simultaneous inactivation of P2X1 and a second protein, α1A-adrenergic receptor, resulted in male infertility.
“Now we know what our therapeutic target looks like, we can generate drugs that can bind to it appropriately, which totally changes the game,” says Ventura.
In 2022, the same team found that extract from the leaves of a stinging nettle (Urtica dioica) blocks P2X1, but not how.
Associate Professor David Thal, also from MIPS, says solving the molecular structure of P2X1 is an important advance for the research group.
“By tapping into state-of-the-art technology we’ve been able to describe the first ever high-resolution structure of P2X1, opening up an exciting new suite of opportunities for developing drugs to target this receptor.”
The research is published in Nature Communications.
