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| What about breast cancer resistance? Scientists propose a new mechanism for drug development |
Science and Technology Daily reporter Chen Xi
Breast cancer is one of the more common malignant tumors in women.
In the pathological classification of breast cancer, about 70% of patients are estrogen receptor (ER)-positive breast cancer, which requires endocrine therapy clinically
.
With the widespread use of ER inhibitors, most patients develop resistance during treatment
Academy of Sciences
According to data from the Globocan website of the International Agency for Research on Cancer of the World Health Organization, China is expected to have about 420,000 new cases of breast cancer and 120,000 deaths in 2021, and the trend is increasing year by year, which is a serious threat to women's health
.
"Of these drug-resistant ER+ breast cancer recurrence patients, about one-third have spontaneously active ER mutations, mainly Y537S and D538G; and in new breast cancer patients, EGFR overexpression will lead to a worse prognosis It is resistant to tamoxifen
In order to solve this problem, Min Jian's research team designed and synthesized a class of dual-mechanism ER inhibitors for the first time
.
In drug design, not only the side chain that plays the role of "direct antagonism" is used, but also specific groups are added to cause indirect antagonism, so that the two different molecular elements of "direct antagonism" and "indirect antagonism" are designed on one ligand.
