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Darolutamide-mediated phospholipid remodeling induces ferroptosis through the SREBP1-FASN axis in prostate cancer

Bingheng Li, Bisheng Cheng, Hao Huang, Shanhe Huang, Shunli Yu, Zean Li, Shirong Peng, Tao Du, Ruihui Xie, Hai Huang

2024International Journal of Biological Sciences27 citationsDOIOpen Access PDF

Abstract

PCa cells. Mechanistically, darolutamide promotes ferroptosis by downregulating SREBP1, which then inhibits the transcription of FASN. FASN knockdown modulates phospholipid remodeling by disrupting the balance between polyunsaturated fatty acids (PUFAs) and saturated fatty acids (SFAs), which induces ferroptosis. Clinically, SREBP1 and FASN are significantly overexpressed in PCa tissues and are related to poor prognosis. Moreover, the synergistic antitumor effect of combination therapy with darolutamide and ferroptosis inducers (FINs) was confirmed in PCa organoids and a mouse xenografts model. Overall, these findings revealed a novel mechanism of darolutamide mediated ferroptosis in PCa, laying the foundation for the combination of darolutamide and FINs as a new therapeutic strategy for PCa patients.

Topics & Concepts

Prostate cancerSterol regulatory element-binding proteinPhospholipidCancerCancer researchProstateBiologyChemistryCell biologyInternal medicineMedicineEndocrinologyBiochemistryCholesterolSterolMembraneCancer, Lipids, and MetabolismFerroptosis and cancer prognosisRNA modifications and cancer
Darolutamide-mediated phospholipid remodeling induces ferroptosis through the SREBP1-FASN axis in prostate cancer | Litcius