ESR1 Y537C

ESR1生物学已成为乳腺癌治疗的核心。在ER+肿瘤中，ESR1配体结合域的突变被证明对激素治疗具有抵抗力。这一证据已导致乳腺癌和卵巢癌中雌激素受体靶向测序的使用增加。Y537C是这些配体结合域突变之一，通常与激素抵抗有关。初步数据表明，ER降解剂，如福尔维斯特，可能有利于治疗ESR1突变，激素抵抗乳腺癌。
ESR1 biology has become a central focus in breast cancer therapy. In ER+ tumors, mutations in the ESR1 ligand binding domain have been shown to confer resistance to hormone therapy. This evidence has led to an increased use of targeted sequencing of the estrogen receptor in breast and ovarian cancer. Y537C is one of these ligand binding domain mutations, and is commonly implicated in this hormone resistance. Preliminary data suggests ER-degrading agents, such as fulvestrant, may be beneficial in treating ESR1 mutant, hormone resistant breast cancers.