ARV-471在雌激素受体阳性乳腺癌治疗中的研究进展

Research progresses of ARV-471 in therapy of estrogen receptor-positive breast cancer

蛋白水解靶向嵌合体(PROTAC)技术是一种新型的靶向蛋白质降解技术,已经广泛应用于疾病相关蛋白的降解,在一定程度上解决了某些调控肿瘤的关键靶点的“不可成药”性和因靶点突变或表达水平增加导致的耐药性。利用这项技术研发出了一种靶向雌激素受体(ER)的口服新药——ARV-471,为ER阳性乳腺癌的治疗提供了新动力。为了促进乳腺癌治疗的进一步发展,本综述就PROTAC应用于转移性ER阳性乳腺癌治疗的可行性和必要性进行分析,为其治疗提供理论基础。

Proteolysis-targeting chimera(PROTAC)technology is a novel targeted protein degradation technology,which has been widely used in the degradation of disease-related proteins.PROTAC has solved the"undrugability"of some key targets regulating tumors and drug resistance caused by mutations or increased expression levels of the targets to a certain extent.ARV-471,an oral new drug targeting estrogen receptor,was developed by using this technology,which provides a new impetus for therapy of estrogen receptor-positive breast cancer.In order to promote the further development of therapy for breast cancer,this review highligts the feasibility and necessity of PROTAC application for the therapy of metastatic estrogen receptor-positive breast cancer,and provides a theoretical basis for treatment of estrogen receptor-positive breast cancer.