AI Article Synopsis
- - The study examines campesterol, a natural phytosterol, as a potential inhibitor of the estrogen receptor α (ERα), which plays a significant role in breast cancer development.
- - Findings show that campesterol effectively binds to ERα, induces conformational changes, and selectively inhibits the growth of ERα-positive breast cancer cells and patient-derived organoids (PDOs).
- - The research suggests that campesterol could be a promising avenue for targeted treatment of ERα-positive breast cancer, highlighting its receptor-specific action.
Article Abstract
Breast cancer remains a global health challenge, and innovative strategies are required to target estrogen receptor α (ERα), a key player in its development. This study investigates the potential of campesterol, a natural phytosterol, as an ERα inhibitor for breast cancer. Our approach integrates , , and experiments to assess the therapeutic potential of campesterol. analyses highlight campesterol as a promising ERα ligand with favorable binding affinities and dynamic properties. Structural analysis reveals conformational changes in ERα upon campesterol binding. studies confirm the selective growth inhibition of campesterol against ERα-positive breast cancer cells. This study extends to ER+ breast cancer patient-derived organoids (PDOs), showing the effectiveness of campesterol in ERα-positive breast cancer PDOs. Importantly, it emphasizes the receptor-specific nature of campesterol, providing insights into its context-dependent action. In conclusion, campesterol displays potential as an ERα inhibitor, offering new avenues for ER+ breast cancer treatment.
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| http://dx.doi.org/10.1021/acs.jmedchem.4c00766 | DOI Listing |
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