New Class of Molecules Developed for Breast Cancer Treatment

Overview of Breast Cancer and Treatment Challenges

American researchers have recently introduced a new class of molecules that may enhance breast cancer treatment options. Breast cancer affects tens of millions of women globally, with over 70% of cases classified as “ER-positive.” This designation indicates that the cancer cells proliferate in response to estrogen. To address this type of breast cancer, doctors typically employ endocrine therapy, which aims to disrupt estrogen receptors in the cancer cells.

Role of Selective Estrogen Receptor Degraders (SERDs)

Selective estrogen receptor degraders (SERDs) are small molecules designed to target and damage the estrogen receptors in cancer cells. This therapeutic approach is often reserved as a last resort for patients facing resistant or metastatic breast cancer. Currently, there is only one SERD approved by the FDA, which necessitates painful injections for delivery. Consequently, researchers are actively seeking new small molecules that can inhibit cancer cell growth and degrade estrogen receptors in breast cancers.

Breakthrough Research Findings

A team of researchers from the United States has developed a promising new class of SERD molecules with significant potential to halt the growth of breast cancer tumors. These molecules feature a unique structure recently identified as effective in obstructing estrogen receptors. Their findings were published in ACS Medicinal Chemistry Letters.

The innovative structure and modular design of the new molecules facilitated the creation of various SERD variations. The researchers conducted tests on 15 of these molecules using breast cancer cells. The experimental results demonstrated that the estrogen receptors within the cells were damaged, and the proliferation of breast cancer cells was significantly slowed when treated with the novel molecules.

Future Research Directions

This research considerably broadens the available options for treating ER-positive breast cancer. Moving forward, the researchers intend to evaluate several of the most promising molecules in mice to advance their development into new breast cancer therapies.

Author Information

Written by Cindi A. Hoover, Ph.D.

References

Wang L, Guillen VS, Sharma N et al. New class of selective estrogen receptor degraders (SERDs): Expanding the toolbox of PROTAC degrons. 2018. ACS Med Chem Lett. 9:803-808. [EurekaAlert!](https://www.eurekalert.org/pub_releases/2018-10/siot-anm100318.php)